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ChEMBL ligand: CHEMBL494753 (Estrone Sulphate) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]