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 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]