Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T58970 | Target Info | |||
| Target Name | Extracellular signal-regulated kinase 2 (ERK2) | ||||
| Synonyms |
PRKM2; PRKM1; P42-MAPK; P42 Mitogen-activated protein kinase; Mitogen-activated protein kinase 2; Mitogen-activated protein kinase 1; MAPK 2; MAPK 1; MAP kinase isoform p42; MAP kinase 2; MAP kinase 1; ERT1; ERK-2
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| Target Type | Clinical trial Target | ||||
| Gene Name | MAPK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Extracellular signal-regulated kinase 1 (ERK1) | Clinical trial Target | ||||
| UniProt ID | MK03_HUMAN | |||||
| Gene Name | MAPK3 | |||||
| Synonyms |
PRKM3; P44-MAPK; P44-ERK1; P44 Mitogen-activated protein kinase; Mitogen-activated protein kinase 3; Microtubule-associated protein-2 kinase; Microtubule-associated protein 2 kinase; MAPK 3; MAP kinase isoform p44; MAP kinase 3; Insulin-stimulated MAP2 kinase; ERT2; ERK-1
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| Representative Drug(s) | GDC-0994 | Drug Info | IC50 = 1.2 nM | [1] | ||
| 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 = 2 nM | [2] | ||
| 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 | [3] | ||
| 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 | [4] | ||
| 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 | [5] | ||
| 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 | [5] | ||
| References | Top | ||||
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| REF 1 | Recent progress on MAP kinase pathway inhibitors. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4047-56. | ||||
| REF 2 | Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3031-4. | ||||
| REF 3 | Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50. | ||||
| REF 4 | 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 5 | 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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