estrone-3-sulphate [Ligand Id: 4749] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL494753 (Estrone Sulphate)
  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
  • This target only has 1 pki data point
1 CHEMBL494753_lig_chart_1 Multidrug resistance-associated protein 1 Human
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  • ABCC4/Multidrug resistance-associated protein 4 in Human [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
  • This target only has 0 pki data point
2 CHEMBL494753_lig_chart_2 Multidrug resistance-associated protein 4 Human
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  • OAT6/Solute carrier family 22 member 20 in Mouse [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
3 CHEMBL494753_lig_chart_3 Solute carrier family 22 member 20 Mouse
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  • Organic anion transporter 3/Solute carrier family 22 member 8 in Rat [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7]
  • This target only has 1 pki data point
4 CHEMBL494753_lig_chart_4 Solute carrier family 22 member 8 Rat
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
  • This target only has 1 pki data point
5 CHEMBL494753_lig_chart_5 Solute carrier organic anion transporter family member 1A1 Rat
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
  • This target only has 1 pki data point
6 CHEMBL494753_lig_chart_6 Solute carrier organic anion transporter family member 1B1 Human
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  • OATP1C1/Solute carrier organic anion transporter family member 1C1 in Mouse [ChEMBL: CHEMBL2073688] [GtoPdb: 1222] [UniProtKB: Q9ERB5]
  • This target only has 1 pki data point
7 CHEMBL494753_lig_chart_7 Solute carrier organic anion transporter family member 1C1 Mouse
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  • Steryl-sulfatase in Human [ChEMBL: CHEMBL3559] [UniProtKB: P08842]
  • This target only has 1 pki data point
8 CHEMBL494753_lig_chart_8 Steryl-sulfatase Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells F 6.35 pKi 450 nM Ki J. Biol. Chem. (2001) 276: 6404-6411 [PMID:11102445]
ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439]
ChEMBL TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells F 4.02 pIC50 95000 nM IC50 Biochem. J. (2003) 371: 361-367 [PMID:12523936]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing Sf9 cells F 4.35 pIC50 45000 nM IC50 Biochem. J. (2003) 371: 361-367 [PMID:12523936]
OAT6/Solute carrier family 22 member 20 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 4.24 pKi 58000 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 4.24 pKi 57543.99 nM Ki J. Biol. Chem. (2007) 282: 23841-23853 [PMID:17553798]
Organic anion transporter 3/Solute carrier family 22 member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7]
ChEMBL TP_TRANSPORTER: inhibition of PCG uptake in OAT3-expressing LLC-PK1 cells F 5.04 pKi 9100 nM Ki Mol. Pharmacol. (2002) 61: 982-988 [PMID:11961115]
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 5.89 pKi 1300 nM Ki Am. J. Physiol. (1996) 270: F326-F331 [PMID:8779894]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in OATP-C-expressing HEK293 cells F 7.34 pKi 45.8 nM Ki Pharm. Res. (2001) 18: 1262-1269 [PMID:11683238]
GtoPdb Measured using estropipate, which is estrone-3-sulfate stabilized with piperazine. - 7.22 pIC50 60 nM IC50 Curr Chem Genomics (2010) 4: 1-8 [PMID:20448812]
OATP1C1/Solute carrier organic anion transporter family member 1C1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073688] [GtoPdb: 1222] [UniProtKB: Q9ERB5]
ChEMBL TP_TRANSPORTER: inhibition of L-T4 uptake in Oatp14-expressing HEK293 cells F 4.27 pKi 53100 nM Ki Endocrinology (2004) 145: 4384-4391 [PMID:15166123]
Steryl-sulfatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559] [UniProtKB: P08842]
ChEMBL Inhibitory activity against steroid sulfatase (STS) desulfation of 4-MUS B 4.22 pKi 60000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 151-155 [PMID:14684318]
ChEMBL Inhibition of steroid sulfatase activity of JEG-3 cells B 5.12 pIC50 7600 nM IC50 J. Med. Chem. (2000) 43: 4465-4478 [PMID:11087571]
ChEMBL Estrone sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S B 5.12 pIC50 7600 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 1891-1896 [PMID:9873454]

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]