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

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ChEMBL ligand: CHEMBL103 (U 3672, Progesta-care, Milprosa, Utrogestan, Prochieve, Progestin, Endometrin, Gesterol, Prometrium, NSC-64377, Cyclogest, Progestasert, Regumate, NSC-9704, Syngestrone, Progesterone, Lutigest, Serenity for women, Crinone)
  • 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