PF-06761281 [Ligand Id: 12850] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3771118
  • Na+/dicarboxylate cotransporter 1/Solute carrier family 13 member 2 in Human [ChEMBL: CHEMBL3712851] [GtoPdb: 978] [UniProtKB: Q13183]
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  • Na+/dicarboxylate cotransporter 3/Solute carrier family 13 member 3 in Human [ChEMBL: CHEMBL3712947] [GtoPdb: 979] [UniProtKB: Q8WWT9]
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  • Na+/citrate cotransporter/Solute carrier family 13 member 5 in Human [ChEMBL: CHEMBL3769293] [GtoPdb: 981] [UniProtKB: Q86YT5]
  • Na+/citrate cotransporter/Solute carrier family 13 member 5 in Mouse [ChEMBL: CHEMBL3769294] [GtoPdb: 981] [UniProtKB: Q67BT3]
  • Na+/citrate cotransporter/Solute carrier family 13 member 5 in Rat [ChEMBL: CHEMBL3769295] [GtoPdb: 981] [UniProtKB: Q8CJ44]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Na+/dicarboxylate cotransporter 1/Solute carrier family 13 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712851] [GtoPdb: 978] [UniProtKB: Q13183]
ChEMBL Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 4.88 pIC50 13200 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 5 pIC50 10000 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
Na+/dicarboxylate cotransporter 3/Solute carrier family 13 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712947] [GtoPdb: 979] [UniProtKB: Q8WWT9]
ChEMBL Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 4.85 pIC50 14100 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 5 pIC50 10000 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
Na+/citrate cotransporter/Solute carrier family 13 member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769293] [GtoPdb: 981] [UniProtKB: Q86YT5]
ChEMBL Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.1 pIC50 794.33 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.13 pIC50 740 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
GtoPdb - - 6.29 pIC50 510 nM IC50 J Med Chem (2016) 59: 1165-75 [PMID:26734723]
ChEMBL Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 6.29 pIC50 510 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis B 6.3 pIC50 501.19 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
Na+/citrate cotransporter/Solute carrier family 13 member 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769294] [GtoPdb: 981] [UniProtKB: Q67BT3]
ChEMBL Inhibition of NaCT in mouse hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.67 pIC50 213.8 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaCT in mouse hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.68 pIC50 210 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
Na+/citrate cotransporter/Solute carrier family 13 member 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769295] [GtoPdb: 981] [UniProtKB: Q8CJ44]
ChEMBL Inhibition of NaCT in rat hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.9 pIC50 125.89 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]
ChEMBL Inhibition of NaCT in rat hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method B 6.92 pIC50 120 nM IC50 J Med Chem (2016) 59: 1165-1175 [PMID:26734723]

ChEMBL data shown on this page come from version 33:

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]