Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T79798 | Target Info | |||
| Target Name | MAP kinase p38 (MAPK12) | ||||
| Synonyms |
Stress-activated protein kinase 3; SAPK3; Mitogen-activated proteinkinase p38 gamma; Mitogen-activated proteinkinase 12; MAPK12; Extracellular signal-regulated kinase 6; ERK6; ERK5; ERK-6
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| Target Type | Successful Target | ||||
| Gene Name | MAPK12 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Stress-activated protein kinase (p38) | Clinical trial Target | ||||
| UniProt ID | MK11_HUMAN; MK12_HUMAN; MK13_HUMAN; MK14_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
p38) Stress-activated protein kinase; P38 MAPK; P38 MAP kinase; Mitogen-activated protein kinase p38
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| Representative Drug(s) | VX-745 | Drug Info | IC50 = 0.8 nM | [1] | ||
| Co-Target Name | Stress-activated protein kinase 2a (p38 alpha) | Clinical trial Target | ||||
| UniProt ID | MK14_HUMAN | |||||
| Gene Name | MAPK14 | |||||
| Synonyms |
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
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| Representative Drug(s) | ARRY-797 | Drug Info | IC50 = 4.5 nM | Click to Show More | [2] | |
| 2 | VX-745 | Drug Info | IC50 = 9 nM | [3] | ||
| Co-Target Name | Proto-oncogene c-RAF (c-RAF) | Clinical trial Target | ||||
| UniProt ID | RAF1_HUMAN | |||||
| Gene Name | RAF1 | |||||
| Synonyms |
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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| Representative Drug(s) | CI-1040 | Drug Info | IC50 = 12 nM | [4] | ||
| Co-Target Name | ERK activator kinase 1 (MEK1) | Clinical trial Target | ||||
| UniProt ID | MP2K1_HUMAN | |||||
| Gene Name | MAP2K1 | |||||
| Synonyms |
PRKMK1; Mitogen-activated protein kinase kinase 1; MKK1; MEK 1; MAPKK 1; MAPK/ERKkinase 1; MAPK/ERK kinase 1; MAP kinase kinase 1; Dual specificity mitogen-activated protein kinase kinase 1
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| Representative Drug(s) | CI-1040 | Drug Info | IC50 = 16 nM | [5] | ||
| Co-Target Name | ERK activator kinase 2 (MEK2) | Clinical trial Target | ||||
| UniProt ID | MP2K2_HUMAN | |||||
| Gene Name | MAP2K2 | |||||
| Synonyms |
PRKMK2; MKK2; MEK 2; MAPKK 2; MAPK/ERK kinase 2; MAP kinase kinase 2; Dual specificity mitogenactivated protein kinase kinase 2; Dual specificity mitogen-activated protein kinase kinase 2
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| Representative Drug(s) | CI-1040 | Drug Info | IC50 = 16 nM | [5] | ||
| Co-Target Name | Casein kinase II alpha (CSNK2A1) | Clinical trial Target | ||||
| UniProt ID | CSK21_HUMAN | |||||
| Gene Name | CSNK2A1 | |||||
| Synonyms |
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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| Representative Drug(s) | CI-1040 | Drug Info | IC50 = 17 nM | [6] | ||
| Co-Target Name | Casein kinase II (CSNK2) | Clinical trial Target | ||||
| UniProt ID | CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | CI-1040 | Drug Info | EC50 = 100 nM | [6] | ||
| Co-Target Name | Stress-activated protein kinase 2b (p38 beta) | Clinical trial Target | ||||
| UniProt ID | MK11_HUMAN | |||||
| Gene Name | MAPK11 | |||||
| Synonyms |
Stress-activated protein kinase-2; SAPK2b; SAPK2; PRKM11; P38b; P38-2; P38 Mitogen-activated protein kinase beta; Mitogen-activated protein kinase p38 beta; Mitogen-activated protein kinase 11; MAPK 11; MAP kinase p38 beta; MAP kinase 11
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| Representative Drug(s) | VX-745 | Drug Info | Ki = 220 nM | [3] | ||
| References | Top | ||||
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| REF 1 | p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5809-13. | ||||
| REF 2 | Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J Med Chem. 2010 Mar 25;53(6):2345-53. | ||||
| REF 3 | The Discovery of VX-745: A Novel and Selective p38alpha Kinase Inhibitor. ACS Med Chem Lett. 2011 Jul 28;2(10):758-63. | ||||
| REF 4 | Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50. | ||||
| REF 5 | 4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase. J Med Chem. 2007 Oct 18;50(21):5090-102. | ||||
| REF 6 | 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. J Med Chem. 2019 Feb 28;62(4):1817-1836. | ||||
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