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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 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]