Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL494753 (Estrone Sulphate) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 32:
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]