CyPPA [Ligand Id: 2323] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL453730 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| KCa2.1/Small conductance calcium-activated potassium channel protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2369] [GtoPdb: 381] [UniProtKB: Q92952] | ||||||||
| ChEMBL | Positive modulation of SK1 (unknown origin) | B | 4 | pEC50 | >100000 | nM | EC50 | Eur J Med Chem (2023) 254: 115353-115353 [PMID:37068385] |
| KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4469] [GtoPdb: 382] [UniProtKB: Q9H2S1] | ||||||||
| ChEMBL | Positive modulation of SK2 (unknown origin) | B | 4.85 | pEC50 | 14000 | nM | EC50 | Eur J Med Chem (2023) 254: 115353-115353 [PMID:37068385] |
| GtoPdb | - | - | 4.9 | pEC50 | - | - | - | Br J Pharmacol (2007) 151: 655-65 [PMID:17486140] |
| KCa2.2/Small conductance calcium-activated potassium channel protein 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2547] [GtoPdb: 382] [UniProtKB: P70604] | ||||||||
| ChEMBL | Potentiation of rat KCa2.2a expressed in HEK293 cells at -90 mV holding potential measured at 1 to 2 days by patch clamp electrophysiology | B | 5.13 | pEC50 | 7480 | nM | EC50 | J Med Chem (2022) 65: 303-322 [PMID:34962403] |
| KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3381] [GtoPdb: 383] [UniProtKB: Q9UGI6] | ||||||||
| ChEMBL | Positive modulation of SK3 (unknown origin) | B | 5.25 | pEC50 | 5600 | nM | EC50 | Eur J Med Chem (2023) 254: 115353-115353 [PMID:37068385] |
| GtoPdb | - | - | 5.3 | pEC50 | - | - | - | Br J Pharmacol (2007) 151: 655-65 [PMID:17486140] |
| KCa2.3/Small conductance calcium-activated potassium channel protein 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3780] [GtoPdb: 383] [UniProtKB: P70605] | ||||||||
| ChEMBL | Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2008) 51: 7625-7634 [PMID:18998663] |
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]
