PIK-75 [Ligand Id: 8012] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL393525 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Inhibition of recombinant human CDK9/cyclin-T1 using H-YSPTSPSYSPTSPSYSPTSPS-KKKK-OH as substrate after 90 mins by luminescence assay | B | 8.86 | pIC50 | 1.37 | nM | IC50 | Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Binding affinity to full length human CDK2 (1 to 298 residues) expressed in bacterial expression system by KINOMEscan competition assay | B | 6.27 | pKd | 540 | nM | Kd | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Binding affinity to full length human CDK7 (1 to 344 residues) expressed in mammalian expression system by KINOMEscan competition assay | B | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Binding affinity to full length human CDK9 (1 to 372 residues) expressed in bacterial expression system by KINOMEscan competition assay | B | 8.39 | pKd | 4.1 | nM | Kd | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Inhibition of human recombinant p110alpha | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522] |
| GtoPdb | - | - | 8.24 | pIC50 | 5.8 | nM | IC50 | Cell (2006) 125: 733-47 [PMID:16647110] |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) by radiometric assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627] |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
| GtoPdb | - | - | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| GtoPdb | - | - | 5.89 | pIC50 | 1300 | nM | IC50 | Cell (2006) 125: 733-47 [PMID:16647110] |
| GtoPdb | - | - | 6.07 | pIC50 | 850 | nM | IC50 | Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739] |
| ChEMBL | Inhibition of human recombinant p110beta | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Inhibition of human recombinant p110delta | B | 6.04 | pIC50 | 910 | nM | IC50 | Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522] |
| GtoPdb | - | - | 6.29 | pIC50 | 510 | nM | IC50 | Cell (2006) 125: 733-47 [PMID:16647110] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay | B | 8.29 | pIC50 | 5.15 | nM | IC50 | Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| GtoPdb | - | - | 7.12 | pIC50 | 76 | nM | IC50 | Cell (2006) 125: 733-47 [PMID:16647110] |
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739] |
| protein kinase, DNA-activated, catalytic subunit in Human [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Cell (2006) 125: 733-47 [PMID:16647110] |
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]
