BTP2 [Ligand Id: 2438] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL262766 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Orai1/Calcium release-activated calcium channel protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384891] [GtoPdb: 2964] [UniProtKB: Q96D31] | ||||||||
| ChEMBL | Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-based FLIPR assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem (2017) 25: 440-449 [PMID:27856238] |
| Orai1/ORAI1/STIM1 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3832645] [GtoPdb: 2964] [UniProtKB: P84903, Q5M848] | ||||||||
| ChEMBL | Inhibition of ORAI/STIM1 in thapsigargin treated rat RBL2H3 cells assessed as reduction in store-operated calcium entry after 5 mins by fura-2-AM dye based assay | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC3/Short transient receptor potential channel 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507] | ||||||||
| ChEMBL | Inhibition of YFP-tagged TRPC3 (unknown origin) expressed in HEK293 cells assessed as reduction carbhocol-induced receptor operated Calcium influx after 5 mins by fura-2-AM dye based assay | B | 5.38 | pIC50 | 4210 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| GtoPdb | - | - | 6.5 | pIC50 | 300 | nM | IC50 | J Biol Chem (2005) 280: 10997-1006 [PMID:15647288] |
| TRPC5/Short transient receptor potential channel 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| ChEMBL | Inhibition of TRPC5 (unknown origin) | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43] | ||||||||
| GtoPdb | - | - | 8.1 | pEC50 | 8 | nM | EC50 | Mol Pharmacol (2006) 69: 1413-20 [PMID:16407466] |
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]
