mifepristone [Ligand Id: 2805] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1276308 (Korlym, Mifegyne, Mifeprex, 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
