Selectivity profile of PH-797804
| PH-797804 Kinase Selectivity (IC50)a | Panlab in Vitro Pharmacology Screen PH-797804 Selectivity (IC50)a | ||||
|---|---|---|---|---|---|
| μM | μM | ||||
| p38α | 0.021 | GSK3β | >10 | PKC | >10 |
| p38β | 0.101 | CK2 | >10 | Fyn | >10 |
| p38γ | >200 | NIM1 | >10 | HER2 | >10 |
| p38δ | >200 | PDGFR | >10 | PKCα | >10 |
| JNK1 | >200 | IR | >10 | PKCg | >10 |
| JNK2 | >200 | PAK4 | >10 | Ca+2/calmodulin protein kinase | >10 |
| JNK3 | >200 | AUR2 | >10 | ERK1 | >10 |
| ERK2 | >200 | PKAα | >10 | ATPase, Na+/K+ | >10 |
| IKK2 | >200 | SULU1 | >10 | ATPase, H+/K+ | >10 |
| IKK1 | >200 | PKCβ | >10 | Phosphodiesterase PDE1 | >10 |
| IKKi | >200 | VEGFR2 | >10 | Phosphodiesterase PDE2 | >10 |
| TBK | >200 | VEGFR3 | >10 | Phosphodiesterase PDE3 | >10 |
| MKK6 | >100 | RET | >10 | Phosphodiesterase PDE4 | >10 |
| MKK7 | >100 | Lyn | >10 | Phosphodiesterase PDE5 | >10 |
| MK-2 | >200 | FGFR1 | >10 | Purinergic P2x | >10 |
| MK-3 | >200 | EGFR1 | >10 | Purinergic P2y | >10 |
| PRAK | >200 | c-MET | >10 | Adenosine A1 | >10 |
| RSK2 | >200 | LCK | >10 | Adenosine A2A | >10 |
| MNK1 | >200 | PDK1 | >10 | Adenosine A3 | >10 |
| MSK1 | 134 | IGFR1 | >10 | 5-HT receptor | >10 |
| CDK2A | >200 | PLK1 | >10 | 5-HT transporter | >10 |
| AKT1 | >10 | STLK | >10 | GLP-1 | >10 |
| CDC7 | >10 | c-ABL | >10 | Glucocorticoid receptor | >10 |
| CHK1 | >10 | ZAP70 | >10 | Monoamine oxidase MAOA | >10 |
| Monoamine oxidase MAOB | >10 | ||||
5-HT, 5-hydroxytryptamine; c-Abl, Abelson murine leukemia viral oncogene homolog; CDC7, cell division cycle protein kinase 7; CHK1, checkpoint kinase-1; CDK2A, cyclin A-associated cyclin-dependent kinase 2; CK2, casein kinase-2; c-MET, mesenchymal-epithelial transition factor receptor; EGFR1, epidermal growth factor receptor; FGFR1, fibroblast growth factor receptor 1; Fyn, fyn tyrosine kinase proto-oncogene; GLP-1, glucagon-like peptide 1; GSK3β, glycogen synthase kinase-3β; HER2, human epidermal growth factor receptor 2; IGFR1, insulin-like growth factor receptor; IKK1, Iκ B kinase 1; IKK2, Iκ B kinase 2; IKKi, inhibitor of κ light polypeptide gene enhancer in B cells, kinase β -inducible; IR, insulin receptor; Lck, lymphocyte-specific protein tyrosine kinase; Lyn, v-yes-1 Yamaguchi sarcoma viral related oncogene homolog; MNK1, mitogen-activated protein kinase-interacting kinase 1; MSK1, mitogen/stress kinase 1; NIM1, new inducer of mitosis 1; PAK4, p21 activated kinase-4; PDGFR, platelet-derived growth factor receptor; PDK1, 3-phosphoinositide-dependent protein kinase-1; PKAα, 3′:5′-AMP-dependent protein kinase α; PKCα, protein kinase C α; PKCβ, protein kinase C β; PKC γ, protein kinase C γ; PLK1, polo-like kinase; PRAK, p38-regulated/activated protein kinase; Ret, rearranged during transfection proto-oncogene; Rsk2, ribosomal protein S6 kinase 2; STLK, Mst3 and SOK1-related kinase; SULU1, Caenorhabditis elegans kinase homolog; TBK, TANK binding kinase; VEGFR2, vascular endothelial growth factor receptor 2; VEGFR3, vascular endothelial growth factor receptor 3; ZAP-70, 70-kDa TCR z-chain-associated protein kinase.
↵a IC50 values are based on enzymatic activity.