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 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]
