mifepristone [Ligand Id: 2805] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1276308 (Korlym, Mifegyne, Mifeprex, Mifepristona, Mifepristone, NSC-759862, RU 38486, RU-38486, RU 486, RU-486, RU486) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 4.92 | pKi | 12082 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 4.58 | pIC50 | 26460 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Alpha trans-inducing protein (VP16) in Herpes simplex virus (type 1 / strain 17) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4218] [UniProtKB: P06492] | ||||||||
| ChEMBL | Antagonistic activity against VP-16 transcriptional activation domain protein | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
| ChEMBL | Binding affinity determined against human Androgen receptor | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation counting | B | 8.08 | pKi | 8.4 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay | B | 8.23 | pKi | 5.95 | nM | Ki | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Displacement of [3H]DHT from human Androgen receptor | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2002) 45: 2417-2424 [PMID:12036351] |
| ChEMBL | Inhibition of human androgen receptor | B | 9.19 | pKi | 0.65 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| GtoPdb | - | - | 9.19 | pKi | 0.65 | nM | Ki | J Med Chem (2004) 47: 4213-30 [PMID:15293993] |
| ChEMBL | Displacement of [3H]mibolerone from human Androgen receptor | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2079-2082 [PMID:15080982] |
| ChEMBL | Binding affinity to AR | B | 7.2 | pIC50 | 63.1 | nM | IC50 | J Med Chem (2010) 53: 4531-4544 [PMID:20469868] |
| ChEMBL | Inhibition of human lymph node carcinoma of prostate (LNCaP) cell proliferation | F | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2004) 47: 4985-4988 [PMID:15456242] |
| ChEMBL | In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor | F | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2000) 43: 5010-5016 [PMID:11150172] |
| ChEMBL | Inhibition of human androgen receptor | B | 8.06 | pIC50 | 8.8 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Inhibition of antagonist activity towards Androgen receptor | F | 8.08 | pIC50 | 8.3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor | B | 8.11 | pIC50 | 7.8 | nM | IC50 | J Med Chem (2004) 47: 4985-4988 [PMID:15456242] |
| ChEMBL | Antagonist activity at androgen receptor ligand binding domain by two hybrid assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4816-4818 [PMID:20638844] |
| ChEMBL | Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| ChEMBL | Antagonist activity at androgen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
| ChEMBL | Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem (2008) 16: 6589-6600 [PMID:18504132] |
| ChEMBL | Antagonist activity against the Androgen Receptor (AR) | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
| ChEMBL | Inhibitory activity against human Androgen receptor | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of human androgen receptor expressed in Escherichia coli | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2004) 47: 4985-4988 [PMID:15456242] |
| ChEMBL | Antagonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay | F | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Agonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
| ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 8.25 | pKi | 5.56 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 8.08 | pIC50 | 8.35 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
| ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 6.26 | pIC50 | 555 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | Inactivation of CYP3A4 (unknown origin) | B | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2020) 63: 5625-5663 [PMID:32031378] |
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Displacement of [3H]E2 from human ERalpha after 16 hrs by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 5.17 | pKi | 6754 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of human Estrogen receptor alpha | B | 6.7 | pKi | >200 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 4.63 | pIC50 | 23638 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at estrogen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
| ChEMBL | Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2008) 16: 6589-6600 [PMID:18504132] |
| ChEMBL | Antagonist activity at estrogen receptor ligand binding domain by two hybrid assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4816-4818 [PMID:20638844] |
| ChEMBL | Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay | F | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Displacement of [3H]E2 from human ERbeta after 16 hrs by scintillation counting | B | 5.54 | pKi | 2876 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Inhibition of human Estrogen receptor beta | B | 6.12 | pKi | >750 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Antagonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay | F | 6.09 | pIC50 | 812 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Agonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Binding affinity to GR (unknown origin) | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem (2019) 27: 2508-2520 [PMID:30929949] |
| GtoPdb | - | - | 9.4 | pKd | - | - | - |
Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004]; J Steroid Biochem (1987) 26: 279-84 [PMID:3560943] |
| ChEMBL | Inhibition of human GR transcriptional activation by HepTAT cells | B | 6.77 | pKi | 169 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 40-44 [PMID:17070047] |
| ChEMBL | Inhibition of glucocorticoid receptor mediated tyrosine amino transferase activity | F | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysis | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2015) 58: 4918-4926 [PMID:25978072] |
| ChEMBL | Inhibition of human GR expressed in hGRAF cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 40-44 [PMID:17070047] |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| ChEMBL | Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression | F | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1312-1317 [PMID:18226897] |
| ChEMBL | Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay | F | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5704-5708 [PMID:17822897] |
| ChEMBL | Displacement of radiolabeled Dexamethasone from human GR | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 40-44 [PMID:17070047] |
| ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 8.99 | pKi | 1.01 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of corticoid-induced transcription by glucocorticoid response element-linked luciferase reporter gene assay | F | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1471-1474 [PMID:17258455] |
| ChEMBL | Displacement of [3H]dexamethasone from human glucocorticoid receptor after 16 hrs by scintillation counting | B | 9.08 | pKi | 0.84 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay | B | 9.09 | pKi | 0.82 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5704-5708 [PMID:17822897] |
| ChEMBL | Binding affinity was determined for human glucocorticoid receptor(hGR). | B | 9.17 | pKi | 0.68 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of glucocorticoid receptor dependent alkaline phosphatase activity | F | 9.36 | pKi | 0.44 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirus | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5704-5708 [PMID:17822897] |
| ChEMBL | Displacement of [3H]dexamethasone from human recombinant GR | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1312-1317 [PMID:18226897] |
| ChEMBL | Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2002) 45: 2417-2424 [PMID:12036351] |
| ChEMBL | Displacement of [3H]DEX from human glucocorticoid receptor | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2010) 53: 3065-3074 [PMID:20334371] |
| ChEMBL | Inhibition of human glucocorticoid receptor | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assay | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (2017) 60: 3405-3421 [PMID:28368581] |
| ChEMBL | Activity at GR in human A549 cells by NF-kappaB transrepression assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 4531-4544 [PMID:20469868] |
| ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2007) 50: 6519-6534 [PMID:18038970] |
| ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay | F | 6 | pIC50 | <1000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
| ChEMBL | Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
| ChEMBL | Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method | B | 7.75 | pIC50 | 17.8 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| ChEMBL | Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method | B | 7.83 | pIC50 | 14.8 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation | F | 7.94 | pIC50 | 11.48 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
| ChEMBL | Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay | B | 8.06 | pIC50 | 8.7 | nM | IC50 | J Med Chem (2018) 61: 1785-1799 [PMID:29424542] |
| ChEMBL | Binding affinity to glucocorticoid receptor | B | 8.16 | pIC50 | 6.92 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
| ChEMBL | Displacement of fluorescent-labeled Dexamethasone from GR by fluorescent polarization assay | B | 8.2 | pIC50 | 6.31 | nM | IC50 | J Med Chem (2010) 53: 4531-4544 [PMID:20469868] |
| ChEMBL | Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induced luciferase transactivation activity after 24 hrs | F | 8.2 | pIC50 | 6.31 | nM | IC50 | J Med Chem (2010) 53: 4531-4544 [PMID:20469868] |
| ChEMBL | Antagonist activity at glucocorticoid receptor expressed in A549 cells assessed as inhibition of corticoid-induced gene transcription by luciferase reporter gene assay | F | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5754-5757 [PMID:17855092] |
| ChEMBL | Inhibition of fluorescent-labeled Dexamethasone binding to GR | B | 8.24 | pIC50 | 5.75 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
| ChEMBL | Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor | B | 8.24 | pIC50 | 5.75 | nM | IC50 | J Med Chem (2007) 50: 6519-6534 [PMID:18038970] |
| ChEMBL | Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2307-2310 [PMID:12824023] |
| ChEMBL | Effect on human Glucocorticoid receptor (GR) in a whole cell assay to measure functional cellular GR-antagonism (GRAF) | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2079-2082 [PMID:15080982] |
| ChEMBL | Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6086-6090 [PMID:16987661] |
| ChEMBL | Antagonistic activity against 5 nM Dexamethasone induced glucocorticoid receptor mediated alkaline phosphatase activity | F | 8.32 | pIC50 | 4.8 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activity | F | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4173-4178 [PMID:15261265] |
| ChEMBL | Inhibition of glucocorticoid receptor Dexamethasone response in reporter gene assay | F | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4179-4183 [PMID:15261266] |
| ChEMBL | Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cells | F | 8.33 | pIC50 | 4.68 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation | F | 8.33 | pIC50 | 4.68 | nM | IC50 | J Med Chem (2007) 50: 6519-6534 [PMID:18038970] |
| ChEMBL | Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2019) 62: 6751-6764 [PMID:31274313] |
| ChEMBL | Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay | B | 8.49 | pIC50 | 3.26 | nM | IC50 | J Med Chem (2019) 62: 6751-6764 [PMID:31274313] |
| ChEMBL | Antagonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
| ChEMBL | Displacement of fluormone tracer from full length human recombinant glucocorticoid receptor expressed in baculovirus expression system incubated for 2 hrs by competitive fluorescence polarization binding assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2019) 62: 6751-6764 [PMID:31274313] |
| ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 8.65 | pIC50 | 2.23 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay | F | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3977-3980 [PMID:19217285] |
| ChEMBL | Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay | F | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2531-2534 [PMID:17317167] |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced GRE-linked luciferase reporter gene activity | F | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 907-910 [PMID:17169557] |
| ChEMBL | Inhibition of Dexamethasone binding to Glucocorticoid receptor | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2307-2310 [PMID:12824023] |
| ChEMBL | Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4173-4178 [PMID:15261265] |
| ChEMBL | Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Binding affinity to human GR | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6086-6090 [PMID:16987661] |
| ChEMBL | Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2079-2082 [PMID:15080982] |
| ChEMBL | Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay | F | 9.02 | pIC50 | 0.95 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Antagonist activity against the Glucocorticoid Receptor (GR) | F | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | Inhibition of antagonist activity towards glucocorticoid receptor | F | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Inhibitory activity against human glucocorticoid receptor (hGR) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luciferase assay | B | 9.19 | pIC50 | 0.64 | nM | IC50 | J Med Chem (2021) 64: 17221-17238 [PMID:34809430] |
| ChEMBL | Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| ChEMBL | Antagonist activity at glucocorticoid receptor ligand binding domain by two hybrid assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4816-4818 [PMID:20638844] |
| ChEMBL | Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2008) 16: 6589-6600 [PMID:18504132] |
| ChEMBL | Antagonist activity at glucocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
| ChEMBL | Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay | B | 9.53 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay | F | 6 | pEC50 | <1000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
| ChEMBL | Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 6.06 | pEC50 | 872 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4761-4769 [PMID:16112571] |
| ChEMBL | Antagonist activity at human GR expressed in CV1 cells by GRE activation assay | F | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2007) 50: 4699-4709 [PMID:17705362] |
| Glucocorticoid receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105966] [UniProtKB: A0A8C0QLS2] | ||||||||
| ChEMBL | Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method | B | 7.49 | pIC50 | 32.6 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method | B | 7.69 | pIC50 | 20.2 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| Glucocorticoid receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295956] [UniProtKB: Q9N1U3] | ||||||||
| ChEMBL | Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method | B | 7.71 | pIC50 | 19.7 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| ChEMBL | Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method | B | 7.96 | pIC50 | 10.9 | nM | IC50 | J Med Chem (2018) 61: 7767-7784 [PMID:30091920] |
| Glucocorticoid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3144] [GtoPdb: 625] [UniProtKB: P06537] | ||||||||
| ChEMBL | In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2000) 43: 5010-5016 [PMID:11150172] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytes | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2307-2310 [PMID:12824023] |
| ChEMBL | Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes | F | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4179-4183 [PMID:15261266] |
| ChEMBL | Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes | F | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4173-4178 [PMID:15261265] |
| ChEMBL | Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-incubated for 1 hr before dexamethasone addition and measured 24 hrs post dexamethasone stimulation by tyrosine aminotransferase enzyme assay | B | 8.71 | pIC50 | 1.94 | nM | IC50 | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Inhibition of [3H]dexamethasone binding to rat glucocorticoid receptor | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Binding affinity to rat glucocorticoid receptor | B | 8.6 | pEC50 | 2.51 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4035-4039 [PMID:17499506] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.09 | pKi | 8038 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 4.7 | pIC50 | 20096 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) | B | 4.08 | pIC50 | 83061 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Displacement of [3H]aldosterone from human mineralocorticoid receptor after 16 hrs by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay | B | 6.07 | pKi | 851 | nM | Ki | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Inhibition of human Mineralocorticoid receptor | B | 6.19 | pKi | 640 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Inhibition of human mineralocorticoid receptor | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Displacement of [3H]aldosterone from human Mineralocorticoid receptor | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2079-2082 [PMID:15080982] |
| ChEMBL | Inhibition of antagonist activity towards mineralocorticoid receptor (hMR) | F | 5.94 | pIC50 | 1155 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Inhibitory activity against human mineralocorticoid receptor (hMR) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Antagonist activity against the Mineralocorticoid Receptor (MR) | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem (2008) 16: 6589-6600 [PMID:18504132] |
| ChEMBL | Antagonist activity at mineralocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
| ChEMBL | Antagonist activity at mineralocorticoid receptor ligand binding domain by two hybrid assay | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4816-4818 [PMID:20638844] |
| ChEMBL | Agonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 6 | pKi | 997 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.61 | pIC50 | 2457 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
| ChEMBL | Compound was tested for the binding affinity towards recombinant NBD2 C-terminal cytotoxic nucleotide-binding domain of mouse P-Glycoprotein | B | 4.7 | pKd | 20000 | nM | Kd | Bioorg Med Chem Lett (2000) 10: 157-160 [PMID:10673101] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Displacement of [3H]-progesterone from cytosolic fraction of human recombinant progesterone-B receptor by scintillation counting analysis | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2015) 58: 4918-4926 [PMID:25978072] |
| ChEMBL | Displacement of radioligand from human Progesterone receptor | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2002) 45: 2417-2424 [PMID:12036351] |
| ChEMBL | Binding affinity at PR by fluorescence binding assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3777-3779 [PMID:16678409] |
| ChEMBL | Displacement of fluorescent ligand from binding domain of progesterone receptor | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3203-3206 [PMID:15925510] |
| ChEMBL | Binding affinity at human progesterone receptor. | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Binding affinity against Baculovirus-Expressed hPR-A | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1998) 41: 3461-3466 [PMID:9719599] |
| ChEMBL | Binding affinity to human progesterone receptor | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
| ChEMBL | Binding affinity against human progesterone receptor-A (hPR-A) | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2731-2736 [PMID:9873612] |
| ChEMBL | Binding affinity towards progesterone receptor was measured | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2747-2750 [PMID:11591515] |
| GtoPdb | - | - | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2071-4 [PMID:12781197] |
| GtoPdb | - | - | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2071-4 [PMID:12781197] |
| ChEMBL | Displacement of [3H]-progesterone from human progesterone receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2015) 58: 6607-6618 [PMID:26218343] |
| ChEMBL | Inhibition of human progesterone receptor | B | 9.19 | pKi | 0.64 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| ChEMBL | Binding affinity determined for human Progesterone receptor A isoform | B | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Inhibition of 4 nM progesterone-stimulated transactivation of MMTV-Luc reporter in CV-1 cells expressing PR-B | F | 9.6 | pKi | 0.25 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3203-3206 [PMID:15925510] |
| ChEMBL | Antagonist activity at progesterone receptor | F | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 723-728 [PMID:22104142] |
| ChEMBL | Binding affinity to PR | B | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2010) 53: 4531-4544 [PMID:20469868] |
| ChEMBL | Displacement of [1,2,6,7-3H]progesterone from recombinant human GST-tagged PGR LBD (678 to 933 residues) expressed in baculovirus-infected insect cells measured after 24 hrs by liquid scintillation counting method | B | 8.28 | pIC50 | 5.2 | nM | IC50 | ACS Med Chem Lett (2018) 9: 641-645 [PMID:30034593] |
| ChEMBL | Inhibition of human progesterone receptor activation in T47D human breast cancer cell. | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| ChEMBL | Displacement of [3H]progesterone from human Progesterone receptor | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2079-2082 [PMID:15080982] |
| ChEMBL | Inhibition of human progesterone receptor | B | 8.54 | pIC50 | 2.9 | nM | IC50 | J Med Chem (2005) 48: 5295-5304 [PMID:16078847] |
| ChEMBL | Inhibition of human progesterone receptor | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4173-4178 [PMID:15261265] |
| ChEMBL | Antagonist activity at progesterone receptor expressed in human T47 cells assessed as blockade of progesterone-induced alkaline phosphatase activity | F | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1471-1474 [PMID:17258455] |
| ChEMBL | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 907-910 [PMID:17169557] |
| ChEMBL | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3977-3980 [PMID:19217285] |
| ChEMBL | Antagonist activity at human progesterone receptor assessed as inhibition of alkaline phosphatase activity in human T47D cells | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2531-2534 [PMID:17317167] |
| ChEMBL | Antagonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc assessed as effect on progesterone-induced activity by luciferase reporter gene assay | F | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| ChEMBL | Antagonistic potency to the human progesterone receptor measured in the T-47D alkaline phosphatase assay | F | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Antagonist activity at human PRB expressed in African green monkey CV1 cells | B | 9.52 | pIC50 | 0.3 | nM | IC50 | ACS Med Chem Lett (2018) 9: 641-645 [PMID:30034593] |
| ChEMBL | Antagonist activity against the Progesterone Receptor (PR) | F | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2731-2736 [PMID:9873612] |
| ChEMBL | Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
| ChEMBL | Inhibitory concentration against progesterone induced PRE-luciferase activity in CV-cells | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2747-2750 [PMID:11591515] |
| ChEMBL | Antagonist activity against progesterone receptor (PR) using PRE-luciferase plasmid co-transfected CV-1 cells | F | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells | F | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1998) 41: 3461-3466 [PMID:9719599] |
| ChEMBL | Antagonist activity against PR beta-mediated transactivation of MMTV luciferase reporter gene in BacMam transduced progesterone-stimulated CV1 cells | F | 9.6 | pIC50 | 0.25 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3777-3779 [PMID:16678409] |
| ChEMBL | Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line | F | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 787-790 [PMID:11859003] |
| ChEMBL | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity | F | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4816-4818 [PMID:20638844] |
| ChEMBL | Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase | F | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2008) 51: 1861-1873 [PMID:18318463] |
| ChEMBL | Inhibitory concentration against progesterone stimulated alkaline phosphatase activity in T47D human breast carcinoma cell line | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2747-2750 [PMID:11591515] |
| ChEMBL | Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells | F | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
| ChEMBL | Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 6589-6600 [PMID:18504132] |
| ChEMBL | Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines. | B | 9.74 | pIC50 | 0.18 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
| ChEMBL | Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. | F | 9.74 | pIC50 | 0.18 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
| ChEMBL | Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line | F | 9.89 | pIC50 | 0.13 | nM | IC50 | J Med Chem (2002) 45: 4379-4382 [PMID:12238914] |
| ChEMBL | Progesterone receptor antagonist activity based on its ability to block progesterone induced alkaline phosphatase in the human breast cancer cell line T47D | F | 10 | pIC50 | 0.1 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 3487-3490 [PMID:12419390] |
| ChEMBL | Antagonist activity at PR in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity measured after 24 hrs | B | 10.14 | pIC50 | 0.07 | nM | IC50 | ACS Med Chem Lett (2018) 9: 641-645 [PMID:30034593] |
| ChEMBL | Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity | F | 10.27 | pIC50 | 0.05 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5754-5757 [PMID:17855092] |
| ChEMBL | Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity | B | 10.3 | pIC50 | 0.05 | nM | IC50 | Bioorg Med Chem (2010) 18: 1891-1898 [PMID:20149664] |
| ChEMBL | Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs | F | 10.35 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2009) 52: 1268-1274 [PMID:19216549] |
| ChEMBL | In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-A progesterone receptor | F | 10.55 | pIC50 | 0.03 | nM | IC50 | J Med Chem (2000) 43: 5010-5016 [PMID:11150172] |
| ChEMBL | In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor | F | 10.6 | pIC50 | 0.03 | nM | IC50 | J Med Chem (2000) 43: 5010-5016 [PMID:11150172] |
| ChEMBL | Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs | F | 10.68 | pIC50 | 0.02 | nM | IC50 | J Med Chem (2009) 52: 1268-1274 [PMID:19216549] |
| ChEMBL | Agonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Antagonistic activity at human progesterone receptor in CV-1 cells. | F | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2075-2078 [PMID:12781198] |
| Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 9.37 | pKi | 0.42 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 8.49 | pIC50 | 3.25 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Progesterone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2596] [GtoPdb: 627] [UniProtKB: Q63449] | ||||||||
| ChEMBL | Inhibition of [3H]R5020 binding to cytosolic progesterone receptor (PRc) of rat uterus | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1899-1902 |
| ChEMBL | Binding affinity to progesterone receptor | B | 7.8 | pEC50 | 15.85 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4035-4039 [PMID:17499506] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 4.96 | pKi | 11047 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 4.58 | pIC50 | 26280 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] | ||||||||
| ChEMBL | Inhibition of human Thyroid hormone receptor alpha | B | 5.9 | pKi | >1250 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
| ChEMBL | Inhibition of human Thyroid hormone receptor beta | B | 5.65 | pKi | >2250 | nM | Ki | J Med Chem (2004) 47: 4213-4230 [PMID:15293993] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 4.67 | pIC50 | 21357 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Pregnane X receptor in Human [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| GtoPdb | - | - | 5 | pEC50 | ~10000 | nM | EC50 | J Clin Invest (1998) 102: 1016-23 [PMID:9727070] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
