corticosterone [Ligand Id: 2869] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL110739 (11-b,21-Dihydroxypregn-3,20-dione, Corticosteron, 17-Deoxycortisol, Corticosterone, Preg-4-ene-3,20-dione,11-b,21-dihydroxy-, NSC-9705)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • 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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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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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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • Glucocorticoid receptor in Mouse [GtoPdb: 625] [UniProtKB: P06537]
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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]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.63 pIC50 23442.29 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
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 4 pKi >100000 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 6.88 pKd 6.88 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 7.2 pKi 63.1 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 7.88 pKi 13.18 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Binding affinity to MR (unknown origin) B 9.3 pKd 0.5 nM Kd J Med Chem (2017) 60: 2629-2650 [PMID:28051871]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 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 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 W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 4.45 pKi 35600 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
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 TEA uptake in OCT1-expressing HeLa cells F 5.15 pKi 7020 nM Ki J. Pharmacol. Exp. Ther. (1998) 286: 354-361 [PMID:9655880]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells F 4.66 pIC50 21700 nM IC50 Br. J. Pharmacol. (2002) 136: 829-836 [PMID:12110607]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake in OCT1-expressing HEK293 cells F 4.14 pKi 72000 nM Ki Naunyn Schmiedebergs Arch. Pharmacol. (1996) 354: 320-326 [PMID:8878062]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes F 5 pKi >10000 nM Ki Nature (1994) 372: 549-552 [PMID:7990927]
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 4.47 pIC50 34200 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 Serotonin uptake in OCT2-expressing HEK293 cells F 6.22 pKi 605 nM Ki J. Biol. Chem. (1998) 273: 30915-30920 [PMID:9812985]
ChEMBL TP_TRANSPORTER: inhibition of Noradrenaline uptake in OCT2-expressing HEK293 cells F 6.34 pKi 460 nM Ki J. Biol. Chem. (1998) 273: 30915-30920 [PMID:9812985]
ChEMBL TP_TRANSPORTER: inhibition of Adrenaline uptake in OCT2-expressing HEK293 cells F 6.38 pKi 420 nM Ki J. Biol. Chem. (1998) 273: 30915-30920 [PMID:9812985]
ChEMBL TP_TRANSPORTER: inhibition of Dopamine uptake in OCT2-expressing HEK293 cells F 6.41 pKi 390 nM Ki J. Biol. Chem. (1998) 273: 30915-30920 [PMID:9812985]
ChEMBL TP_TRANSPORTER: inhibition pramipexole uptake in rOCT2-injected oocytes F 4.97 pIC50 10700 nM IC50 Drug Metab. Dispos. (2005) 33: 495-499 [PMID:15640376]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT2-expressing HRPE cells F 5.38 pIC50 4200 nM IC50 J. Biol. Chem. (1998) 273: 32776-32786 [PMID:9830022]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in Xenopus laevis oocytes F 5.4 pIC50 4000 nM IC50 Am. J. Physiol. Renal Physiol. (2001) 281: F454-F468 [PMID:11502595]
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 6.54 pIC50 290 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 5.31 pIC50 4900 nM IC50 J. Biol. Chem. (1998) 273: 32776-32786 [PMID:9830022]
Solute carrier organic anion transporter family member 1A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing HeLa cells F 5.28 pKi 5300 nM Ki Am. J. Physiol. (1996) 270: F326-F331 [PMID:8779894]
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
ChEMBL Binding affinity towards human testosterone binding globulin. B 5.34 pKd 5.34 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin B 6.34 pKd 457.09 nM Kd J. Med. Chem. (2008) 51: 2047-2056 [PMID:18330978]
Glucocorticoid receptor in Mouse [GtoPdb: 625] [UniProtKB: P06537]
GtoPdb - - 7.2 pIC50 - - - Eur. J. Pharmacol. (1993) 247: 145-54 [PMID:8282004];
FEBS Lett. (1999) 464: 9-13 [PMID:10611474];
J. Biol. Chem. (2000) 275: 19041-9 [PMID:10747884]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]