Cobimetinib

drug
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Also known as Gdc 0623Gdc 0973Gdc-0623GDC-0973RG 7420RG-7420RG7420Xl 518Xl518

Summary

Cobimetinib (CHEMBL2146883) is an approved small-molecule EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor (ATC L01EE02) targeting MAP2K1, MAP2K2, and MAP2K7; indicated across 26 conditions including neoplasm and melanoma; with CIViC clinical evidence for 17 variant-indication associations (e.g. BRAF V600 in melanoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EE02
  • Targets: 3 (MAP2K1, MAP2K2, MAP2K7)
  • Indications: 26 conditions
  • Clinical trials: 107
  • Precision-oncology evidence (CIViC): 17 variant–indication associations
  • Chemistry: 531.3 Da · C21H21F3IN3O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2146883
NameCobimetinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID16222096
ChEBICHEBI:90851
ATCL01EE02
Molecular formulaC21H21F3IN3O2
Molecular weight531.3
InChIKeyBSMCAPRUBJMWDF-KRWDZBQOSA-N

SMILES: C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O

IUPAC name: [3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone

ChEBI definition: A member of the class of N-acylazetidines obtained by selective formal condensation of the carboxy group of 3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzoic acid with the secondary amino group from the azetidine ring of 3-[(2S)-piperidin-2-yl]azetidin-3-ol. An inhibitor of mitogen-activated protein kinase that is used (as its fumarate salt) in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma.

Pharmacological roles (ChEBI): EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, antineoplastic agent.

Also known as: Cobimetinib, Gdc 0623, Gdc 0973, Gdc-0623, GDC-0973, RG 7420, RG-7420, RG7420, Xl 518, Xl518, COBIMETINIB, cobimetinib

Parent form; salt/anhydrous children: CHEMBL2364607, CHEMBL3526209

Patent coverage: 3,767 distinct patent families (9,422 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,229 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
MAP2K1mitogen-activated protein kinase kinase 1Negative9.054.7%Q02750
MAP2K2mitogen-activated protein kinase kinase 2Negative6.73.1%P36507
MAP2K7mitogen-activated protein kinase kinase 7Negative53.9%O14733

Broader ChEMBL bioactivity targets: 16 (assay-derived). Sample: D(1A) dopamine receptor, Thromboxane A2 receptor, Muscarinic acetylcholine receptor M2, Dual specificity mitogen-activated protein kinase kinase; MEK1/2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, D(3) dopamine receptor.

Bioactivity

ChEMBL activities: 21 potent at pChembl ≥ 5 of 28 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
MAP2K29.7IC500.2nMCHEMBL_ACT_12041238
MAP2K19.7IC500.2nMCHEMBL_ACT_29186985
MAP2K19.05IC500.9nMCHEMBL_ACT_12041220
MAP2K19.05IC500.9nMCHEMBL_ACT_26186113
MAP2K19.05IC500.9nMCHEMBL_ACT_29186981
BRAF8.74IC501.8nMCHEMBL_ACT_15461647
MAP2K18.38IC504.2nMCHEMBL_ACT_15461649
MAP2K18.38IC504.2nMCHEMBL_ACT_24954265
MAP2K18.38IC504.2nMCHEMBL_ACT_25564478
MAP2K18.38IC504.2nMCHEMBL_ACT_26276968
MAP2K18.18IC506.6nMCHEMBL_ACT_29065673
MAP2K27.66Kd22nMCHEMBL_ACT_17910662
MAP2K27.64IC5023nMCHEMBL_ACT_24957049
MAP2K17.51IC5031nMCHEMBL_ACT_24957048
ACTR37.44Kd36nMCHEMBL_ACT_17880444
ACTR37.28IC5053nMCHEMBL_ACT_24957047
OPRM16.57AC50271.4nMCHEMBL_ACT_25158356
MAP2K16.51Kd309nMCHEMBL_ACT_17910460
KCNH25.89AC501300nMCHEMBL_ACT_25117961
SLC6A35.14AC507295nMCHEMBL_ACT_25125140
SLC6A45.11AC507824nMCHEMBL_ACT_25151508

Target pathways

Aggregated over 3 target gene(s): MAP2K1, MAP2K2, MAP2K7.

Top Reactome pathways

69 total, by targets touching each:

PathwayTargetsGenes
Disease3MAP2K1, MAP2K2, MAP2K7
Uptake and function of anthrax toxins3MAP2K1, MAP2K2, MAP2K7
Uptake and actions of bacterial toxins3MAP2K1, MAP2K2, MAP2K7
Infectious disease3MAP2K1, MAP2K2, MAP2K7
Bacterial Infection Pathways3MAP2K1, MAP2K2, MAP2K7
RAF-independent MAPK1/3 activation2MAP2K1, MAP2K2
Developmental Biology2MAP2K1, MAP2K2
Cytokine Signaling in Immune system2MAP2K1, MAP2K7
Signal Transduction2MAP2K1, MAP2K2
Toll Like Receptor 4 (TLR4) Cascade2MAP2K1, MAP2K7
MyD88:MAL(TIRAP) cascade initiated on plasma membrane2MAP2K1, MAP2K7
MyD88-independent TLR4 cascade2MAP2K1, MAP2K7
Signaling by NTRKs2MAP2K1, MAP2K2
Toll Like Receptor 9 (TLR9) Cascade2MAP2K1, MAP2K7
Toll Like Receptor 10 (TLR10) Cascade2MAP2K1, MAP2K7
Toll Like Receptor 3 (TLR3) Cascade2MAP2K1, MAP2K7
Toll Like Receptor 5 (TLR5) Cascade2MAP2K1, MAP2K7
Toll Like Receptor TLR1:TLR2 Cascade2MAP2K1, MAP2K7
Toll Like Receptor 7/8 (TLR7/8) Cascade2MAP2K1, MAP2K7
Toll Like Receptor TLR6:TLR2 Cascade2MAP2K1, MAP2K7
Innate Immune System2MAP2K1, MAP2K7
Immune System2MAP2K1, MAP2K7
Toll-like Receptor Cascades2MAP2K1, MAP2K7
Prolonged ERK activation events2MAP2K1, MAP2K2
Frs2-mediated activation2MAP2K1, MAP2K2
Toll Like Receptor 2 (TLR2) Cascade2MAP2K1, MAP2K7
Signaling by NTRK1 (TRKA)2MAP2K1, MAP2K2
Signalling to ERKs2MAP2K1, MAP2K2
L1CAM interactions2MAP2K1, MAP2K2
Axon guidance2MAP2K1, MAP2K2

Dominant GO biological processes

GO termTargets
positive regulation of DNA-templated transcription3
protein phosphorylation3
MAPK cascade2
signal transduction2
heart development2
positive regulation of gene expression2
Schwann cell development2
thyroid gland development2
regulation of stress-activated MAPK cascade2
ERBB2-ERBB3 signaling pathway2
myelination2
insulin-like growth factor receptor signaling pathway2
thymus development2
regulation of axon regeneration2
positive regulation of axonogenesis2

Indications & clinical

Indications

26 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
melanoma3MONDO:0005105EFO:0000756
cutaneous melanoma3MONDO:0005012EFO:0000389
metastatic melanoma3MONDO:0005191EFO:0002617
colorectal carcinoma3MONDO:0024331EFO:1001951
colorectal neoplasm3MONDO:0005335MONDO:0005575
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
craniopharyngioma2MONDO:0018907EFO:1000209
breast neoplasm2MONDO:0021100MONDO:0007254
breast carcinoma2MONDO:0004989EFO:0000305
chronic myelomonocytic leukemia2MONDO:0020311EFO:1001779
thyroid gland carcinoma2MONDO:0015075EFO:0002892
gallbladder carcinoma2MONDO:0003220EFO:1001956
arteriovenous malformations of the brain2MONDO:0007154Orphanet:46724
lymphoid neoplasm2MONDO:0005157EFO:0001642
acute myeloid leukemia1MONDO:0018874EFO:0000222
gastric adenocarcinoma1MONDO:0005036EFO:0000503
plasma cell myeloma1MONDO:0009693EFO:0001378
sarcoma1MONDO:0005089EFO:0000691
carcinoma of esophagus1MONDO:0019086EFO:0002916
ovarian cancer1MONDO:0008170MONDO:0008170
skin neoplasm1MONDO:0002531MONDO:0002898
adenocarcinoma1MONDO:0004970MONDO:0003219
exocrine pancreatic carcinoma0MONDO:0005192EFO:0002618
pancreatic ductal adenocarcinoma0MONDO:0005184MONDO:0005184

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 107.

Phase distribution

PhaseTrials
PHASE247
PHASE131
PHASE1/PHASE214
PHASE37
Not specified4
PHASE2/PHASE32
EARLY_PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03178552PHASE2/PHASE3ACTIVE_NOT_RECRUITINGA Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC)
NCT03768063PHASE3ACTIVE_NOT_RECRUITINGA Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study
NCT05768178PHASE2/PHASE3RECRUITINGDETERMINE Trial Treatment Arm 05: Vemurafenib in Combination With Cobimetinib in Adult Patients With BRAF Positive Cancers.
NCT01689519PHASE3COMPLETEDA Study Comparing Vemurafenib Versus Vemurafenib Plus Cobimetinib in Participants With Metastatic Melanoma
NCT02427893PHASE3WITHDRAWNTrial of Vemurafenib and Cobimetinib in Patients With Advanced BRAFV600 Mutant Melanoma
NCT02788279PHASE3COMPLETEDA Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma (COTEZO IMblaze370)
NCT02908672PHASE3COMPLETEDA Study of Atezolizumab Plus Cobimetinib and Vemurafenib Versus Placebo Plus Cobimetinib and Vemurafenib in Previously Untreated BRAFv600 Mutation-Positive Patients With Metastatic or Unresectable Locally Advanced Melanoma
NCT03273153PHASE3TERMINATEDA Study of Cobimetinib Plus Atezolizumab Versus Pembrolizumab in Participants With Previously Untreated Advanced BRAFv600 Wild-Type Melanoma
NCT04007848PHASE3COMPLETEDCobimetinib for BRAF-wild-type or Mutated Histiocytoses
NCT02693535PHASE2RECRUITINGTAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
NCT03175432PHASE2ACTIVE_NOT_RECRUITINGBevacizumab and Atezolizumab With or Without Cobimetinib in Treating Patients With Untreated Melanoma Brain Metastases
NCT03181100PHASE2ACTIVE_NOT_RECRUITINGAtezolizumab With Chemotherapy in Treating Patients With Anaplastic or Poorly Differentiated Thyroid Cancer
NCT03202316PHASE2ACTIVE_NOT_RECRUITINGAtezolizumab, Cobimetinib, and Eribulin in Treating Patients With Chemotherapy Resistant Metastatic Inflammatory Breast Cancer
NCT03202940PHASE1/PHASE2ACTIVE_NOT_RECRUITINGA Phase IB/II Study of Alectinib Combined With Cobimetinib in Advanced ALK-Rearranged (ALK+) NSCLC
NCT03224767PHASE2ACTIVE_NOT_RECRUITINGVemurafenib and Cobimetinib in Treating Patients With BRAF V600E Mutation Positive Craniopharyngioma
NCT03600701PHASE2ACTIVE_NOT_RECRUITINGAtezolizumab and Cobimetinib in Treating Patients With Metastatic, Recurrent, or Refractory Non-small Cell Lung Cancer
NCT04079179PHASE2RECRUITINGCobimetinib in Refractory Langerhans Cell Histiocytosis (LCH), and Other Histiocytic Disorders
NCT04185831PHASE2ACTIVE_NOT_RECRUITINGA MolEcularly Guided Anti-Cancer Drug Off-Label Trial
NCT04302025PHASE2RECRUITINGA Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC)
NCT04409639PHASE2ACTIVE_NOT_RECRUITINGCobimetinib in Newly Diagnosed or HMA-treated CMML Patients With RAS Pathway Mutations
NCT04931342PHASE2ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors
NCT04941287PHASE2ACTIVE_NOT_RECRUITINGTesting A New Combination of Anti-cancer Immune Therapies, Atezolizumab and CDX-1127 (Varlilumab) With or Without the Addition of a Third Anti-cancer Drug, Cobimetinib, for Advanced-Stage Biliary Tract Cancer
NCT05159245PHASE2RECRUITINGThe Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs
NCT06440850PHASE2RECRUITINGVemurafenib and Cobimetinib for the Treatment of Patients With High Risk Differentiated Thyroid Carcinoma With BRAFV600E Mutation
NCT06813079PHASE2NOT_YET_RECRUITINGUsing Tumor Models to Determine Treatments
NCT07449754PHASE2RECRUITINGBelvarafenib in Combination With Cobimetinib in Patients With Locally Advanced or Metastatic NRAS-Mutant Melanoma
NCT01495988PHASE2TERMINATEDTrial of Vemurafenib/Cobimetinib With or Without Bevacizumab in Patients With Stage IV BRAFV600 Mutant Melanoma
NCT01813214PHASE2TERMINATEDThe Effects of Vemurafenib + Cobimetinib on Immunity in Patients With Melanoma
NCT01928394PHASE1/PHASE2COMPLETEDA Study of Nivolumab by Itself or Nivolumab Combined With Ipilimumab in Patients With Advanced or Metastatic Solid Tumors
NCT01959633PHASE1/PHASE2COMPLETEDVemurafenib Plus Cobimetinib Plus PEG-interferon in Advanced Melanoma Patients Harboring the V600BRAF Mutation
NCT02036086PHASE2UNKNOWNStudy of Neo-adjuvant Use of Vemurafenib Plus Cobimetinib for BRAF Mutant Melanoma With Palpable Lymph Node Metastases
NCT02060188PHASE2COMPLETEDA Study of Nivolumab Alone or Nivolumab Combination Therapy in Colon Cancer That Has Come Back or Has Spread
NCT02091141PHASE2COMPLETEDMy Pathway: A Study Evaluating Herceptin/Perjeta, Tarceva, Zelboraf/Cotellic, Erivedge, Alecensa, and Tecentriq Treatment Targeted Against Certain Molecular Alterations in Participants With Advanced Solid Tumors
NCT02230306PHASE2TERMINATEDPhase II Study of Cobimetinib in Combination With Vemurafenib in Active Melanoma Brain Metastases
NCT02291289PHASE2COMPLETEDA Study of Biomarker-Driven Therapy in Metastatic Colorectal Cancer (mCRC)
NCT02303951PHASE2TERMINATEDNeoadjuvant Vemurafenib + Cobimetinib + Atezolizumab in Melanoma: NEO-VC
NCT02322814PHASE2TERMINATEDA Study of Cobimetinib Plus Paclitaxel, Cobimetinib Plus Atezolizumab Plus Paclitaxel, or Cobimetinib Plus Atezolizumab Plus Nab-Paclitaxel as Initial Treatment for Participants With Triple-Negative Breast Cancer That Has Spread
NCT02537600PHASE2COMPLETEDVemurafenib and Cobimetinib Combination in BRAF Mutated Melanoma With Brain Metastasis
NCT02583516PHASE2COMPLETEDClinical Trial to Evaluate the Efficacy of Vemurafenib in Combination With Cobimetinib (Continuous and Intermittent) in BRAFV600-mutation Positive Patients With Unresectable Locally Advanced or Metastatic Melanoma
NCT02639546PHASE1/PHASE2COMPLETEDSafety and Pharmacokinetics of Cobimetinib in Pediatric and Young Adult Participants With Previously Treated Solid Tumors

Clinical evidence (CIViC)

Variant × indication × effect (17 predictive associations from 18 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
BRAF V600MelanomaSensitivity/ResponseCobimetinib + VemurafenibCIViC AEID6044 +1
BRAF V600MelanomaSensitivity/ResponseAtezolizumab + Vemurafenib + CobimetinibCIViC AEID11238
ARAF MutationLangerhans-cell HistiocytosisSensitivity/ResponseCobimetinibCIViC BEID11297
ARAF Mutation AND ARAF S225V AND ARAF P216AErdheim-Chester DiseaseSensitivity/ResponseCobimetinibCIViC BEID11296
BRAF Non-V600Erdheim-Chester DiseaseSensitivity/ResponseCobimetinibCIViC BEID11298
BRAF Non-V600Langerhans-cell HistiocytosisSensitivity/ResponseCobimetinibCIViC BEID11299
BRAF V600MelanomaSensitivity/ResponseVemurafenib + CobimetinibCIViC BEID1422
BRAF V600EMelanomaSensitivity/ResponseCobimetinib + VemurafenibCIViC BEID1421
BRAF V600E OR BRAF K601EColorectal CancerSensitivity/ResponseCobimetinib + VemurafenibCIViC BEID11670
NRAS Mutation OR KRAS Mutation OR RAF1 Mutation OR MAP2K1 Mutation OR MAP2K2 MutationErdheim-Chester DiseaseSensitivity/ResponseCobimetinibCIViC BEID11328
NRAS Mutation OR KRAS Mutation OR RAF1 Mutation OR MAP2K1 Mutation OR MAP2K2 MutationLangerhans-cell HistiocytosisSensitivity/ResponseCobimetinibCIViC BEID11329
BRAF V600EGangliogliomaSensitivity/ResponseVemurafenib + CobimetinibCIViC CEID11310
BRAF V600E AND CDKN2A Deletion AND CDKN2B Deletion AND TET2 E796K AND BAX L76R AND AXIN2 P455KGangliogliomaSensitivity/ResponseCobimetinib + VemurafenibCIViC CEID11314
GOLGA4::RAF1 FusionMelanomaSensitivity/ResponseTrametinib + CobimetinibCIViC CEID8374
KRAS G12RHistiocytosis-Lymphadenopathy Plus SyndromeSensitivity/ResponseCobimetinibCIViC CEID7310
KRAS G12R AND GATA3 Mutation AND GNAS MutationHistiocytosis-Lymphadenopathy Plus SyndromeSensitivity/ResponseCobimetinibCIViC CEID11330
BRAF V600ECancerSensitivity/ResponseCobimetinibCIViC DEID1141

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

77 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AXITINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
BOSUTINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
FEDRATINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
RUXOLITINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
SELUMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
SORAFENIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
SUNITINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
VANDETANIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
VEMURAFENIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
NERATINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2, MAP2K7
CANERTINIBChEMBLPhase 3MAP2K1, MAP2K2, MAP2K7
LESTAURTINIBChEMBLPhase 3MAP2K1, MAP2K2, MAP2K7
AfatinibPubChemApprovedMAP2K1, MAP2K2, MAP2K7
CrizotinibPubChemApprovedMAP2K1, MAP2K2, MAP2K7
GefitinibPubChemApprovedMAP2K1, MAP2K2, MAP2K7
IdelalisibPubChemApprovedMAP2K1, MAP2K2, MAP2K7
PazopanibPubChemApprovedMAP2K1, MAP2K2, MAP2K7
BINIMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
LapatinibChEMBL + PubChemPhase 4 (approved)MAP2K2, MAP2K7
TRAMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
DASATINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
GILTERITINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
NINTEDANIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
AVUTOMETINIBChEMBLPhase 3MAP2K1, MAP2K2
DOVITINIBChEMBLPhase 3MAP2K1, MAP2K2
LINSITINIBChEMBLPhase 3MAP2K1, MAP2K2
ORANTINIBChEMBLPhase 3MAP2K1, MAP2K2
SARACATINIBChEMBLPhase 3MAP2K1, MAP2K2
CENISERTIBChEMBLPhase 2MAP2K1, MAP2K2
CEP-32496ChEMBLPhase 2MAP2K1, MAP2K2
CI-1040ChEMBLPhase 2MAP2K1, MAP2K2
DEFOSBARASERTIBChEMBLPhase 2MAP2K1, MAP2K2
FORETINIBChEMBLPhase 2MAP2K1, MAP2K2
ILORASERTIBChEMBLPhase 2MAP2K1, MAP2K2
MIRDAMETINIBChEMBLPhase 2MAP2K1, MAP2K2
PELITINIBChEMBLPhase 2MAP2K1, MAP2K2
PIMASERTIBChEMBLPhase 2MAP2K1, MAP2K2
R-406ChEMBLPhase 2MAP2K1, MAP2K2
REFAMETINIBChEMBLPhase 2MAP2K1, MAP2K2
SU-014813ChEMBLPhase 2MAP2K1, MAP2K2
TAK-733ChEMBLPhase 2MAP2K1, MAP2K2
TOZASERTIBChEMBLPhase 2MAP2K1, MAP2K2
dacomitinibPubChemApprovedMAP2K1, MAP2K2
ErlotinibPubChemApprovedMAP2K2, MAP2K7
FostamatinibPubChemApprovedMAP2K1, MAP2K2
IbrutinibPubChemApprovedMAP2K2, MAP2K7
ImatinibPubChemApprovedMAP2K2, MAP2K7
QuizartinibPubChemApprovedMAP2K2, MAP2K7
regorafenibPubChemApprovedMAP2K1, MAP2K2
TOFACITINIBChEMBLPhase 4 (approved)MAP2K1
CEDIRANIBChEMBLPhase 3MAP2K2
LINIFANIBChEMBLPhase 3MAP2K2
BIIB-091ChEMBLPhase 2MAP2K2
E-6201ChEMBLPhase 2MAP2K1
SCH-900776ChEMBLPhase 2MAP2K2
SOTRASTAURINChEMBLPhase 2MAP2K1
TOLONIUM CHLORIDEChEMBLPhase 2MAP2K1
ZAPNOMETINIBChEMBLPhase 2MAP2K1
BaricitinibPubChemApprovedMAP2K2
CabozantinibPubChemApprovedMAP2K2