phenylglycine-01 [Ligand Id: 4284] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1949980 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569] | ||||||||
| ChEMBL | Potentiation of CFTR F508del mutant (unknown origin) expressed in CHO cells assessed as chloride transport by measuring membrane potential incubated for 5 to 30 mins in presence of forskolin by Quattro assay | B | 5.9 | pEC50 | 1250 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
| ChEMBL | Potentiation of wild-type CFTR (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin | B | 6 | pEC50 | 990 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
| ChEMBL | Potentiation of CFTR F508del mutant (unknown origin) expressed in CHO cells assessed as chloride transport by measuring membrane potential preincubated for 5 mins followed by forskolin addition by FLIPR assay | B | 6.41 | pEC50 | 390 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
| ChEMBL | Potentiation of CFTR F508del mutant (unknown origin) expressed in FRT cells assessed as chloride transport by measuring membrane potential in presence of forskolin | B | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (2021) 64: 7241-7260 [PMID:34028270] |
| CFTR/Cystic fibrosis transmembrane conductance regulator in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3992] [GtoPdb: 707] [UniProtKB: P34158] | ||||||||
| ChEMBL | Potentiation of CFTR F508del mutant in rat FRT cells assessed as increase in iodide influx in presence of forskolin | B | 7.15 | pEC50 | 70 | nM | EC50 | Eur J Med Chem (2020) 204: 112631-112631 [PMID:32898816] |
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]
