PF-06649298 [Ligand Id: 12849] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3769578 |
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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 | pIC50 | >100000 | 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 | pIC50 | >100000 | 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 | 4.79 | pIC50 | 16200 | nM | IC50 | J Med Chem (2016) 59: 1165-1175 [PMID:26734723] |
| ChEMBL | Inhibition of SLC13A5 in human hepatocyte cells assessed as reduction in citrate uptake | B | 4.79 | pIC50 | 16200 | nM | IC50 | J Med Chem (2023) 66: 9229-9250 [PMID:37428122] |
| ChEMBL | Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method | B | 4.8 | pIC50 | 15848.93 | 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] |
| ChEMBL | Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2016) 59: 1165-1175 [PMID:26734723] |
| GtoPdb | - | - | 6.4 | pIC50 | 400 | nM | IC50 | Sci Rep (2015) 5: 17391 [PMID:26620127] |
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]
