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 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]