AC1903 [Ligand Id: 10290] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1345058 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPC4/Short transient receptor potential channel 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295971] [GtoPdb: 489] [UniProtKB: Q9UBN4] | ||||||||
| ChEMBL | Inhibition of human TRPC4 channel expressed in HEK293 cells assessed as inhibition of EA-evoked Calcium influx by measuring reduction in intracellular Ca2+ level and measured upto 360 sec by Fluo-4/AM dye based FLIPR assay | B | 4.11 | pIC50 | 77200 | nM | IC50 | Bioorg Med Chem (2022) 68: 116853-116853 [PMID:35653869] |
| TRPC5/Short transient receptor potential channel 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| ChEMBL | Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as inhibition of EA-evoked Calcium influx by measuring reduction in intracellular Ca2+ level and measured upto 360 sec by Fluo-4/AM dye based FLIPR assay | B | 4.19 | pIC50 | 64970 | nM | IC50 | Bioorg Med Chem (2022) 68: 116853-116853 [PMID:35653869] |
| GtoPdb | Inhibition of riluzole-activated TRPC5 whole-cell current by patch-clamp recording. | - | 4.83 | pIC50 | 14700 | nM | IC50 | Science (2017) 358: 1332-1336 [PMID:29217578] |
| TRPC5/Short transient receptor potential channel 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523481] [GtoPdb: 490] [UniProtKB: Q9QX29] | ||||||||
| ChEMBL | Inhibition of mouse TRPC5 expressed in Flp-In-T-Rex-HEK293 cells assessed as reduction in rulizole-induced channel current by automated patch clamp method | B | 5.39 | pIC50 | 4060 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 155-159 [PMID:30538066] |
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]
