progesterone [Ligand Id: 2377] activity data from GtoPdb and ChEMBL

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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)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • Acyl coenzyme A:cholesterol acyltransferase 1 in Human [ChEMBL: CHEMBL2782] [UniProtKB: P35610]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • fatty acid binding protein 2/Fatty acid binding protein intestinal in Human [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
  • Organic cation transporter 3/Solute carrier family 22 member 3 in Rat [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
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  • CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]
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  • CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3]
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  • CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]