5604 |
MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1 |
MAP2K1 |
CFC3 |
MAPKK1 |
MEK1 |
MKK1 |
PRKMK1 |
176872 |
6840 |
ENSG00000169032 |
OTTHUMG00000133196 |
Dual specificity mitogen-activated protein kinase kinase 1 |
ERK activator kinase 1 |
MAPK/ERK kinase 1 |
MAP kinase kinase 1 |
MAPKK 1 |
MEK 1 |
BE0000870 |
Q02750 |
2062 |
NM_002755 |
NP_002746 |
31 |
MP2K1_HUMAN |
DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1 (EC 2.7.1.-) (MAP KINASE KINASE 1) (MAPKK 1) (ERK ACTIVATOR KINASE 1) (MAPK/ERK KINASE 1) (MEK1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q02750] |
MEK |
T35940 |
GuideToPharmacology Gene Category Name | STE7 family |
GuideToPharmacology Gene Category ID | 623 |
Interpro Name | Serine/threonine- / dual-specificity protein kinase, catalytic domain |
Interpro Acc | IPR002290 |
Human Readable Name | DRUGGABLE GENOME |
Uniprot Status | Swiss-Prot |
Interpro Type | Domain |
Interpro Short Name | Ser/Thr_dual-sp_kinase_dom |
Human Readable Name | KINASE |
Uniprot Evidence | 1: Evidence at protein level |
CancerCommons Reported Gene Name | MEK |
Target Class | Enzymes |
Target Subclass | EC:2.7.12.2 |
Gene Biotype | PROTEIN_CODING |
KINASE |
SERINE THREONINE KINASE |
TYROSINE KINASE |
DRUG RESISTANCE |
NUCLEAR HORMONE RECEPTOR |
DRUGGABLE GENOME |
CLINICALLY ACTIONABLE |
ENZYME |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Reported Cancer Type | Melanoma |
inhibitor (inhibitory) |
Reported Cancer Type | Melanoma |
allosteric modulator |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Novel drug target | Novel Target |
inhibitor (inhibitory) |
Indication/Tumor Type | melanoma |
Response Type | resistant |
Approval Status | Preclinical |
allosteric modulator |
inhibitor (inhibitory) |
Specific Action of the Ligand | Negative |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
Details of the Assay for Interaction | Measured in a fluorescence anisotropy assay using recombinant MEK1. Ki approximated from the graph in supplementary figure 1b. |
allosteric modulator |
inhibitor (inhibitory) |
Specific Action of the Ligand | Negative |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
Trial Name | AZD-8330 |
Novel drug target | Novel Target |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
allosteric modulator |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Reported Cancer Type | Melanoma |
inhibitor (inhibitory) |
Evidence Type | Actionable |
Approval Status | Preclinical |
Response Type | sensitive |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Trial Name | GSK1120212 |
Novel drug target | Novel Target |
Notes |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Notes | |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
allosteric modulator |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Negative |
n/a |
Trial Name | ARRY-300 |
Novel drug target | Novel Target |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
Reported Cancer Type | Melanoma |
inhibitor (inhibitory) |
Trial Name | WX-554 |
Novel drug target | Novel Target |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
allosteric modulator |
inhibitor (inhibitory) |
Indication/Tumor Type | melanoma |
Response Type | resistant |
Approval Status | Preclinical - Cell culture |
inhibitor (inhibitory) |
Mechanism of Interaction | Dual specificity mitogen-activated protein kinase kinase 1 inhibitor |
Direct Interaction | yes |
MAP2K1 | Ensembl Gene Name |
Gene Biotype | PROTEIN_CODING |
Q02750 | Uniprot Accession |
MP2K1_HUMAN | Uniprot Id |
5604 | Entrez Gene Id |
Interpro Name | Serine/threonine- / dual-specificity protein kinase, catalytic domain |
Interpro Acc | IPR002290 |
Human Readable Name | DRUGGABLE GENOME |
KINASE, DRUGGABLE GENOME |
DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1 (EC 2.7.1.-) (MAP KINASE KINASE 1) (MAPKK 1) (ERK ACTIVATOR KINASE 1) (MAPK/ERK KINASE 1) (MEK1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q02750] | Description |
ENSG00000169032 | Ensembl Gene Id |
MAP2K1 | Display Id |
Human Readable Name | DRUGGABLE GENOME |
DRUGGABLE GENOME |
5604 | Entrez Gene ID |
CancerCommons Reported Gene Name | MEK |
MAP2K1 | Gene Symbol |
Target Class | Enzymes |
Target Subclass | EC:2.7.12.2 |
6840 | HUGO Gene ID |
6840 | HUGO Gene Symbol |
mitogen-activated protein kinase kinase 1 | HUGO Gene Name |
GuideToPharmacology Gene Category Name | STE7 family |
GuideToPharmacology Gene Category ID | 623 |
ENZYME |
5604 | CKB Entrez Id |
MAP2K1 | CKB Gene Synonym |
CFC3 | CKB Gene Synonym |
5604 | Entrez Gene ID |
31 | CIViC Gene ID |
DRUG RESISTANCE |
MAP2K1 | DrugBank Gene Name |
Q02750 | UniProt Accession |
5604 | Entrez Gene Id |
ENSG00000169032 | Gene Symbol |
MAP2K1 | Ensembl Id |
DRUGGABLE GENOME |
5604 | Entrez Gene Id |
MAP2K1 | MyCancerGenome Gene Symbol |
MEK | MyCancerGenome Reported Gene Name |
MEK1 | Gene Symbol |
PRKMK1 | GENE_SYMBOL |
MEK1 | GENE_SYMBOL |
MAP2K1 | GENE_SYMBOL |
5604 | OncoKB Entrez Id |
MKK1 | OncoKB Gene Synonym |
PRKMK1 | OncoKB Gene Synonym |
Dual specificity mitogen-activated protein kinase kinase 1 | Gene Name |
Q02750 | UniProt ID |
KINASE, NUCLEAR HORMONE RECEPTOR |
MEK1 | GO Gene Synonym |
PRKMK1 | GO Gene Synonym |
SERINE THREONINE KINASE, TYROSINE KINASE |
MAP2K1 | Gene Symbol |
CLINICALLY ACTIONABLE |
5604 | Gene ID |
MAPKK1 | dGene Synonym |
MEK1 | dGene Synonym |
KINASE, SERINE THREONINE KINASE |
MEK1 | TTD Gene Abbreviation |
T35940 | TTD Target ID |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
DRUG RESISTANCE |