compound 4 [PMID: 24432870] [Ligand Id: 8941] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3128046 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
| ChEMBL | Binding affinity to N-terminal GST-His-tagged recombinant human PAK1 kinase domain expressed in Escherichia coli BL21 using KKRNRRLSVA as sustrate preincubated for 10 mins followed by ATP addition measured after 60 mins by FRET-based Z'Lyte assay | B | 5.35 | pKi | >4500 | nM | Ki | J Med Chem (2014) 57: 1033-1045 [PMID:24432870] |
| GtoPdb | - | - | 5.35 | pKi | 4500 | nM | Ki |
ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365]; J Med Chem (2014) 57: 1033-45 [PMID:24432870] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Binding affinity to N-terminal GST-tagged recombinant human PAK4 kinase domain expressed in Escherichia coli using KKRNRRLSVA as substrate preincubated for 10 mins followed by ATP addition measured after 60 mins by FRET-based Z'Lyte assay | B | 5.54 | pKi | >2900 | nM | Ki | J Med Chem (2014) 57: 1033-1045 [PMID:24432870] |
| GtoPdb | - | - | 8.12 | pIC50 | 7.5 | nM | IC50 | ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365] |
| p21 (RAC1) activated kinase 2 in Human [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| GtoPdb | - | - | 6.01 | pIC50 | 970 | nM | IC50 | ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365] |
| p21 (RAC1) activated kinase 3 in Human [GtoPdb: 2135] [UniProtKB: O75914] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365] |
| p21 (RAC1) activated kinase 6 in Human [GtoPdb: 2137] [UniProtKB: Q9NQU5] | ||||||||
| GtoPdb | - | - | 6.9 | pIC50 | 126 | nM | IC50 | ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365] |
| p21 (RAC1) activated kinase 5 in Human [GtoPdb: 2138] [UniProtKB: Q9P286] | ||||||||
| GtoPdb | - | - | 7.44 | pIC50 | 36 | nM | IC50 | ACS Med Chem Lett (2015) 6: 776-81 [PMID:26191365] |
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]
