PF-3644022 [Ligand Id: 8045] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1231206 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PRKAA1 | B | 6.93 | pIC50 | 117 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2016) 59: 3609-3634 [PMID:26502061] |
| BR serine/threonine kinase 1/BR serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c BRSK1 | B | 6.73 | pIC50 | 187 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c BRSK2 | B | 7.05 | pIC50 | 90 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| calcium/calmodulin-dependent protein kinase II beta subunit/CaM kinase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CAMK2B | B | 7.15 | pIC50 | 70 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CDK1 | B | 6.45 | pIC50 | 354 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CDK5 | B | 6.04 | pIC50 | 902 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Inhibition of recombinant MK2 (45 to 400 residues) (unknown origin) using fluorescein isothiocyanate-KKKALSRQLSVAA as substrate | B | 8.3 | pKi | 5 | nM | Ki | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| GtoPdb | - | - | 8.52 | pKi | 3 | nM | Ki | J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073] |
| ChEMBL | Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis | B | 6.7 | pIC50 | 201 | nM | IC50 | J Med Chem (2016) 59: 3609-3634 [PMID:26502061] |
| ChEMBL | Affinity On-target Cellular interaction (Western Blot (phosphorylation of the MK2 substrate HSP27 in U937 cells)) EUB0000056c MAPKAPK2 | B | 6.7 | pIC50 | 201 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK2 | F | 6.8 | pIC50 | 159 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| GtoPdb | - | - | 8.28 | pIC50 | 5.2 | nM | IC50 | J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073] |
| ChEMBL | Binding affinity to recombinant MAPKAP-K2 using KKKALSRQLSVAA as substrate after 4 mins by surface plasmon resonance spectroscopic analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 6700-6715 [PMID:22746295] |
| ChEMBL | Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK2 | B | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of human MK2 | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2021) 64: 1283-1345 [PMID:33481605] |
| MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK3 | F | 6.8 | pIC50 | 159 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK3 | B | 7.28 | pIC50 | 53 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK5 | F | 6.8 | pIC50 | 159 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK5 | B | 8.3 | pIC50 | 5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MKNK2 | B | 6.83 | pIC50 | 148 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MAP3K5 | B | 7.22 | pIC50 | 60 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PHKG2 | B | 6.28 | pIC50 | 528 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MERTK | B | 7.12 | pIC50 | 76 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| serine/threonine kinase 17a/Serine/threonine-protein kinase 17A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4525] [GtoPdb: 2214] [UniProtKB: Q9UEE5] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c STK17A | B | 7.15 | pIC50 | 71 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PIM1 | B | 7.06 | pIC50 | 88 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c RIPK2 | B | 6.23 | pIC50 | 590 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c AXL | B | 6.37 | pIC50 | 428 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
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]
