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ChEMBL ligand: CHEMBL103 (Crinone, Cyclogest, Endometrin, Gesterol, Lutigest, Milprosa, NSC-64377, NSC-9704, Prochieve, Progesta-care, Progestasert, Progesterone, Progesterone, micronized, Progesteronum, Progestin, Prometrium, Regumate, Serenity for women, Syngestrone, U 3672, Utrogestan) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125] | ||||||||
ChEMBL | Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
Acyl coenzyme A:cholesterol acyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2782] [UniProtKB: P35610] | ||||||||
ChEMBL | In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (1986) 29: 1131-1133 [PMID:3100794] |
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation counting | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
ChEMBL | Binding affinity against baculovirus expressed human androgen receptor (hAR) | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1999) 42: 1466-1472 [PMID:10212133] |
ChEMBL | Binding affinity for human Androgen receptor | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Displacement of DHT from human androgen receptor expressed in baculovirus SF-12 cells | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Binding affinity against human androgen receptor | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Binding affinity was determined on Human androgen receptor (hAR) using progesterone as radioligand. | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | Displacement of DHT from human androgen receptor | B | 8.07 | pKi | 8.5 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
ChEMBL | Inhibition of human androgen receptor at 10e-12 to 10e-5 M | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Antagonist activity against Androgen receptor | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
ChEMBL | Inhibitory activity against human Androgen receptor | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Inhibitory activity (IC50) against human androgen receptor expressed in CV-1 cells | F | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Antagonistic activity was determined in Human androgen receptor(hAR) of CV-1 cells in cotransfection assay. | F | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay | B | 7.86 | pIC50 | 13.7 | nM | IC50 | Eur J Med Chem (2019) 171: 265-281 [PMID:30925341] |
Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
ChEMBL | Inhibitory activity against Androgen receptor | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1313-1316 [PMID:12657271] |
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 | 6.84 | pKi | 143 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 6.67 | pIC50 | 214 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
ChEMBL | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) | F | 4.76 | pIC50 | 17300 | nM | IC50 | Pharm Res (2003) 20: 537-544 [PMID:12739759] |
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352] | ||||||||
ChEMBL | Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | B | 5.35 | pKi | 4430 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185] | ||||||||
ChEMBL | In silico binding affinity to human corticosteriod binding globulin | B | 6.38 | pKd | 6.38 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
ChEMBL | Binding affinity to human CBG receptor (corticosteroid-binding globulins) | B | 7.38 | pKi | 41.69 | nM | Ki | J Med Chem (2004) 47: 2732-2742 [PMID:15139751] |
ChEMBL | Binding affinity to the corticosteroid-binding globulin (CBG) receptor. | B | 7.38 | pKi | 7.38 | mM | Log Ki | J Med Chem (2000) 43: 3233-3243 [PMID:10966742] |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | Binding affinity for human Estrogen receptor Alpha | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2005) 48: 3463-3466 [PMID:15887952] |
ChEMBL | Binding affinity for human Estrogen receptor Alpha | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2005) 48: 3463-3466 [PMID:15887952] |
fatty acid binding protein 2/Fatty acid binding protein intestinal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104] | ||||||||
ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP | B | 4.7 | pKi | 20000 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692] | ||||||||
ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 6.82 | pKi | 150 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity against baculovirus expressed human glucocorticoid receptor (hGR) | B | 7.52 | pKi | 30.5 | nM | Ki | J Med Chem (1999) 42: 1466-1472 [PMID:10212133] |
ChEMBL | Binding affinity was determined for human glucocorticoid receptor(hGR). | B | 7.52 | pKi | 30.5 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Displacement of Dexamethasone from human glucocorticoid receptor expressed in baculovirus SF-12 cells | B | 7.52 | pKi | 30.5 | nM | Ki | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Binding affinity against human glucocorticoid receptor expressed in SF-12 cells | B | 7.52 | pKi | 30.5 | nM | Ki | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Binding affinity was determined on Human glucocorticoid receptor (hAR) using progesterone as radioligand. | B | 7.52 | pKi | 30.5 | nM | Ki | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | Displacement of Dexamethasone from human glucocorticoid receptor | B | 7.52 | pKi | 30.5 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
ChEMBL | Inhibition of human glucocorticoid receptor at 10e-12 to 10e-5 M | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Inhibitory activity against GR (glucocorticoid receptor) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1313-1316 [PMID:12657271] |
ChEMBL | Antagonist activity at glucocorticoid (hGR) receptor; not active | F | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
ChEMBL | Inhibitory activity against human glucocorticoid receptor (hGR) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Inhibitory activity (IC50) against human glucocorticoid receptor expressed in CV-1 cells | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Antagonistic activity was determined in Human glucocorticoid receptor(hGR) of CV-1 cells in cotransfection assay. | F | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 6.48 | pIC50 | 330 | nM | IC50 | DrugMatrix in vitro pharmacology data |
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6] | ||||||||
ChEMBL | Agonist activity at human TGR5 expressed in CHO cells by luciferase assay | F | 5.56 | pEC50 | 2770 | nM | EC50 | J Med Chem (2008) 51: 1831-1841 [PMID:18307294] |
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
ChEMBL | Affinity for recombinant Mineralocorticoid receptor | B | 9.41 | pKd | 0.39 | nM | Kd | J Med Chem (1996) 39: 2860-2864 [PMID:8709117] |
ChEMBL | Inhibition of 10e-9 M aldosterone activity in CV-1 cells expressing mineralocorticoid receptor | F | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1996) 39: 2860-2864 [PMID:8709117] |
ChEMBL | Inhibitory activity against human Mineralocorticoid receptor | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Antagonist activity at mineralocorticoid receptor (hMR) | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
ChEMBL | Inhibitory activity against human mineralocorticoid receptor (hMR) | B | 7.85 | pIC50 | >14 | nM | IC50 | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Inhibitory activity (IC50) against human mineralocorticoid receptor expressed in CV-1 cells | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Antagonistic activity was determined in Human mineralocorticoid receptor(hMR) of CV-1 cells in cotransfection assay. | F | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
GtoPdb | - | - | 11 | pIC50 | - | - | - | Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004] |
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373] | ||||||||
ChEMBL | Antagonist activity at human P2X3 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced calcium flux measured for 30 secs at 0.4 secs intervals by Flou-4-AM dye based fluorescence assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2018) 151: 462-481 [PMID:29649742] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | F | 4.02 | pIC50 | 96200 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells | F | 4.06 | pIC50 | 88100 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | Inhibition of P-glycoprotein by Hoechst assay | B | 4.31 | pIC50 | 48977.88 | nM | IC50 | Bioorg Med Chem (2007) 15: 7470-7479 [PMID:17890094] |
ChEMBL | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay | B | 4.32 | pIC50 | 47863.01 | nM | IC50 | Bioorg Med Chem (2007) 15: 7470-7479 [PMID:17890094] |
ChEMBL | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay | B | 4.32 | pIC50 | 47863.01 | nM | IC50 | Bioorg Med Chem (2008) 16: 8224-8236 [PMID:18678495] |
ChEMBL | TP_TRANSPORTER: reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells | F | 4.67 | pEC50 | 21200 | nM | EC50 | J Med Chem (2002) 45: 390-398 [PMID:11784143] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 4.62 | pIC50 | 24000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 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 GB4 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 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 7G8 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 HB3 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] |
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
ChEMBL | Displacement of [3H]progesterone from human progesterone receptor B after 16 hrs by scintillation counting | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
ChEMBL | Binding affinity for human progesterone receptor isoform A expressed in CV-1 cells | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1998) 41: 2779-2785 [PMID:9667968] |
ChEMBL | Binding affinity against human progesterone receptor (hPR) in a competitive binding assay | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
ChEMBL | Binding affinity to human progesterone receptor | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
ChEMBL | Binding affinity determined for human Progesterone receptor A isoform | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | Binding affinity was determined against hPR-A (human progesterone receptor) using progesterone radioligand in competitive binding assay | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
ChEMBL | Binding affinity towards human progesterone receptor A isoform using progesterone as radioligand | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Binding affinity against human progesterone receptor | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | The binding affinity on Human progesterone receptor (hPR-A) using progesterone as radioligand. | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | The binding affinity measured using baculovirus-expressed hPR-A in sf21 cells. | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1998) 41: 303-310 [PMID:9464361] |
ChEMBL | Binding affinity against baculovirus expressed human Progesterone receptor | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1999) 42: 1466-1472 [PMID:10212133] |
GtoPdb | - | - | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | Displacement of [3H]progesterone from Progesterone receptor | B | 8.46 | pKi | 3.47 | nM | Ki | J Med Chem (2006) 49: 4261-4268 [PMID:16821785] |
ChEMBL | Binding affinity at human progesterone receptor | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2008) 51: 3696-3699 [PMID:18553958] |
ChEMBL | Antagonistic activity was determined in Human progesterone receptor(hPR) of CV-1 cells in cotransfection assay. | F | 5 | pIC50 | <10000 | nM | IC50 | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
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 | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
ChEMBL | Binding affinity against Progesterone receptor in human TE85 osteosarcoma cells was determined using (Z)-[125I]-17-alpha-(2-iodovinyl)-19-nor-testosterone as radioligand | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1995) 38: 4880-4884 [PMID:8523400] |
ChEMBL | Binding affinity towards human progesterone receptor | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1995) 38: 4878-4879 [PMID:8523399] |
ChEMBL | Binding affinity for Progesterone receptor (PR) in human T47D breast carcinoma cells | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 787-790 [PMID:11859003] |
ChEMBL | Binding affinity to progesterone receptor | B | 9.7 | pIC50 | 0.2 | nM | IC50 | ACS Med Chem Lett (2011) 2: 124-129 [PMID:24900290] |
ChEMBL | Antagonist activity against hPR (human progesterone receptor) compared to that of progesterone (100%) | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
ChEMBL | Agonist activity at human PR | B | 7.3 | pEC50 | 50 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
ChEMBL | Agonist activity at PR (unknown origin) by Alpha Screen assay | B | 7.3 | pEC50 | 50 | nM | EC50 | Medchemcomm (2019) 10: 1412-1419 [PMID:31673308] |
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 | 7.82 | pEC50 | 15.2 | nM | EC50 | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
ChEMBL | Effective concentration (EC50) against human progesterone receptor expressed in CV-1 cell | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (1998) 41: 4354-4359 [PMID:9784110] |
ChEMBL | Effective concentration for agonist activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells | F | 8.54 | pEC50 | 2.9 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2071-2074 [PMID:12781197] |
ChEMBL | Agonistic activity against human progesterone receptor in CV-1 cells | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Agonist activity was determined against hPR (human progesterone receptor) compared to that of progesterone (100%) | F | 8.54 | pEC50 | 2.9 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 3365-3370 [PMID:9873735] |
ChEMBL | Compound was tested for agonistic activity by cotransfection assay against human Progesterone receptor in CV-1 cells | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (1999) 42: 1466-1472 [PMID:10212133] |
ChEMBL | Agonistic activity to the human progesterone receptor (hPR)assayed in CV-1 cells in cotransfection assay. | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (1998) 41: 291-302 [PMID:9464360] |
ChEMBL | Human progesterone receptor (hPR) agonist activity expressed in CV-1 cells | F | 8.54 | pEC50 | 2.9 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
ChEMBL | Agonistic activity was measured for modulation of hPR-B (human progesterone receptor) in co-transfected CV-1 cells. | F | 8.54 | pEC50 | 2.89 | nM | EC50 | J Med Chem (1998) 41: 303-310 [PMID:9464361] |
ChEMBL | Agonist activity at human progesterone receptor in human T47D cells assessed as alkaline phosphatase activity | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2008) 51: 3696-3699 [PMID:18553958] |
ChEMBL | Agonist activity at human PRGR expressed in HEK293 cells by luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
ChEMBL | Human progesterone receptor (hPR) agonist activity in T47D human breast cancer cell line | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 415-418 [PMID:10743938] |
ChEMBL | Agonistic activity against human progesterone receptor in T47D breast cancer cells | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2003) 46: 4104-4112 [PMID:12954062] |
ChEMBL | Agonistic activity by cotransfection assay against human Progesterone receptor in T47D cells | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (1999) 42: 1466-1472 [PMID:10212133] |
GtoPdb | - | - | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (1998) 41: 2779-85 [PMID:9667968] |
ChEMBL | Effective concentration for half-maximal activation of human progesterone receptor expressed in CV-1 cells | B | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (1998) 41: 2779-2785 [PMID:9667968] |
ChEMBL | Agonistic activity against progesterone receptor in alkaline phosphatase assay using human T47D breast carcinoma cell line | F | 9.04 | pEC50 | 0.92 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 787-790 [PMID:11859003] |
ChEMBL | Effective concentration against PR (progesterone receptor) | B | 9.04 | pEC50 | 0.92 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1313-1316 [PMID:12657271] |
ChEMBL | Effective concentration on alkaline phosphatase activity in human T47D breast carcinoma cell line. | F | 9.05 | pEC50 | 0.9 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1313-1316 [PMID:12657271] |
ChEMBL | Activity at progesterone receptor assessed as alkaline phosphatase activity in human T47D cells | B | 9.05 | pEC50 | 0.9 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5015-5017 [PMID:18722119] |
ChEMBL | Agonist activity at human progesterone receptor | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2008) 51: 3696-3699 [PMID:18553958] |
ChEMBL | Agonist activity at PR in human T47D cells using p-nitrophenyl phosphate as substrate assessed as induction of alkaline phosphatase activity incubated for 72 hrs followed by substrate addition measured after 24 hrs by alkaline phosphatase assay | B | 9.74 | pEC50 | 0.18 | nM | EC50 | Bioorg Med Chem (2021) 49: 116425-116425 [PMID:34607200] |
ChEMBL | Activation of progesterone receptor in human T47D cells after 20 hrs by PRE-tagged luciferase reporter gene assay | B | 10 | pEC50 | 0.1 | nM | EC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 8.44 | pKi | 3.62 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 7.55 | pIC50 | 28 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Progesterone receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3456] [UniProtKB: P06186] | ||||||||
ChEMBL | Inhibition of [3H]R5020 binding to rabbit uterine progesterone receptor | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1985) 28: 1695-1699 [PMID:4067997] |
ChEMBL | Displacement of [3H]progesterone from rabbit PR by liquid scintillation counting | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
ChEMBL | Displacement of [3H]progesterone from progesterone receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis | B | 6.18 | pKi | 661 | nM | Ki | Bioorg Med Chem (2013) 21: 1844-1856 [PMID:23462714] |
ChEMBL | Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting | B | 6.18 | pKi | 660 | nM | Ki | J Med Chem (2011) 54: 6704-6713 [PMID:21859078] |
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 | 5.89 | pKi | 1284 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2005) 48: 4754-4764 [PMID:16033255] |
ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 5.51 | pIC50 | 3055 | nM | IC50 | DrugMatrix in vitro pharmacology data |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
ChEMBL | Displacement of [3H]pentazocine from sigma-1 opioid receptor in rat liver membranes after 1 hr by liquid scintillation spectrometric analysis | B | 6.62 | pKd | 239 | nM | Kd | J Med Chem (2013) 56: 7137-7160 [PMID:23734634] |
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells | F | 5.52 | pIC50 | 3050 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells | F | 4.57 | pIC50 | 26700 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT2-expressing HRPE cells | F | 5.8 | pIC50 | 1600 | nM | IC50 | J Biol Chem (1998) 273: 32776-32786 [PMID:9830022] |
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells | F | 5.37 | pIC50 | 4280 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
Organic cation transporter 3/Solute carrier family 22 member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT3-expressing HRPE cells | F | 4.98 | pIC50 | 10500 | nM | IC50 | J Biol Chem (1998) 273: 32776-32786 [PMID:9830022] |
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278] | ||||||||
ChEMBL | Binding affinity towards human testosterone binding globulin. | B | 5.94 | pKd | 5.94 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
ChEMBL | Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | B | 6.94 | pKd | 114.82 | nM | Kd | J Med Chem (2008) 51: 2047-2056 [PMID:18330978] |
CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5] | ||||||||
GtoPdb | Patch clamp electrophysiology, kinetic rapid mixing fluorometry, 2-3 µM shows the saturating efficacy. | - | 8.11 | pEC50 | 7.7 | nM | EC50 |
Nature (2011) 471: 387-91 [PMID:21412339]; Nature (2011) 471: 382-6 [PMID:21412338] |
CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56] | ||||||||
GtoPdb | Patch clamp electrophysiology, kinetic rapid mixing fluorometry; 2-3 µM shows the saturating efficacy. | - | 8.11 | pEC50 | 7.7 | nM | EC50 |
Nature (2011) 471: 387-91 [PMID:21412339]; Nature (2011) 471: 382-6 [PMID:21412338] |
CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3] | ||||||||
GtoPdb | Patch clamp electrophysiology, kinetic rapid mixing fluorometry, 2-3µM shows the saturating efficacy. | - | 8.11 | pEC50 | 7.7 | nM | EC50 |
Nature (2011) 471: 387-91 [PMID:21412339]; Nature (2011) 471: 382-6 [PMID:21412338] |
CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7] | ||||||||
GtoPdb | Patch clamp electrophysiology, kinetic rapid mixing fluorometry, 2-3µM shows the saturating efficacy. | - | 8.11 | pEC50 | 7.7 | nM | EC50 |
Nature (2011) 471: 387-91 [PMID:21412339]; Nature (2011) 471: 382-6 [PMID:21412338] |
TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - | Br J Pharmacol (2011) 162: 1509-20 [PMID:21108630] |
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]