Trametinib

drug
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Also known as GSK-1120212GSK1120212JTP 74057JTP-74057MekinistTMT-212Tmt212GSK1120212BTRAMETINIB DIMETHYL SULFOXIDECPD 8BGSK 1120212TRAMETINIB (GSK1120212)SID137276024

Summary

Trametinib (CHEMBL2103875) is an approved small-molecule EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor (ATC L01EE01) targeting MAP2K1 and MAP2K2; indicated across 52 conditions including neoplasm and melanoma; with CIViC clinical evidence for 134 variant-indication associations (e.g. BRAF V600E in pleomorphic xanthoastrocytoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EE01
  • Targets: 2 (MAP2K1, MAP2K2)
  • Indications: 52 conditions
  • Clinical trials: 251
  • Precision-oncology evidence (CIViC): 134 variant–indication associations
  • Chemistry: 615.4 Da · C26H23FIN5O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2103875
NameTrametinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11707110
ChEBICHEBI:75998
ATCL01EE01
Molecular formulaC26H23FIN5O4
Molecular weight615.4
InChIKeyLIRYPHYGHXZJBZ-UHFFFAOYSA-N

SMILES: CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5

IUPAC name: N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide

ChEBI definition: A pyridopyrimidine that is used (as its dimethyl sulfoxide addition compound) for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, and who have not received prior BRAF inhibitor treatment.

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

Also known as: GSK-1120212, GSK1120212, JTP 74057, JTP-74057, Mekinist, TMT-212, Tmt212, TMT212, Trametinib, TRAMETINIB, GSK1120212B, TRAMETINIB DIMETHYL SULFOXIDE

Parent form; salt/anhydrous children: CHEMBL2105741

Patent coverage: 5,853 distinct patent families (14,034 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 13,631 (97%) 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 1Inhibition9.154.7%Q02750
MAP2K2mitogen-activated protein kinase kinase 2Inhibition8.743.1%P36507

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Dual specificity mitogen-activated protein kinase kinase; MEK1/2, Dual specificity mitogen-activated protein kinase kinase 2, Dual specificity mitogen-activated protein kinase kinase 1, ATP-dependent translocase ABCB1.

Bioactivity

ChEMBL activities: 43 potent at pChembl ≥ 5 of 43 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
MAP2K19.32IC500.48nMCHEMBL_ACT_25754167
MAP2K29.32IC500.48nMCHEMBL_ACT_25754177
MAP2K19.28IC500.52nMCHEMBL_ACT_25754168
MAP2K29.28IC500.52nMCHEMBL_ACT_25754178
MAP2K19.15IC500.7nMCHEMBL_ACT_19449815
MAP2K19.04IC500.92nMCHEMBL_ACT_24788473
MAP2K19.04IC500.92nMCHEMBL_ACT_24788639
MAP2K29.04IC500.92nMCHEMBL_ACT_25755755
MAP2K28.8IC501.6nMCHEMBL_ACT_13972310
MAP2K28.8IC501.6nMCHEMBL_ACT_25778537
MAP2K28.74IC501.8nMCHEMBL_ACT_24788474
MAP2K28.74IC501.8nMCHEMBL_ACT_24788642
MAP2K18.74IC501.8nMCHEMBL_ACT_25755754
MAP2K28.7IC502nMCHEMBL_ACT_24789081
MAP2K28.67IC502.16nMCHEMBL_ACT_29048786
MAP2K18.66IC502.2nMCHEMBL_ACT_25754176
MAP2K28.66IC502.2nMCHEMBL_ACT_25754186
MAP2K18.64IC502.3nMCHEMBL_ACT_25754174
MAP2K28.64IC502.3nMCHEMBL_ACT_25754184
MAP2K18.47IC503.4nMCHEMBL_ACT_13972311
MAP2K18.47IC503.4nMCHEMBL_ACT_25778535
MAP2K18.39IC504.1nMCHEMBL_ACT_25754172
MAP2K28.39IC504.1nMCHEMBL_ACT_25754182
MAP2K18.24IC505.7nMCHEMBL_ACT_25754171
MAP2K28.24IC505.7nMCHEMBL_ACT_25754181
MAP2K18.07IC508.5nMCHEMBL_ACT_25754173
MAP2K28.07IC508.5nMCHEMBL_ACT_25754183
MAP2K28.05Kd9nMCHEMBL_ACT_17910570
MAP2K27.9IC5012.7nMCHEMBL_ACT_26329357
MAP2K27.83IC5014.9nMCHEMBL_ACT_19449816

Target pathways

Aggregated over 2 target gene(s): MAP2K1, MAP2K2.

Top Reactome pathways

62 total, by targets touching each:

PathwayTargetsGenes
RAF-independent MAPK1/3 activation2MAP2K1, MAP2K2
Developmental Biology2MAP2K1, MAP2K2
Signal Transduction2MAP2K1, MAP2K2
Disease2MAP2K1, MAP2K2
Signaling by NTRKs2MAP2K1, MAP2K2
Prolonged ERK activation events2MAP2K1, MAP2K2
Frs2-mediated activation2MAP2K1, MAP2K2
Signaling by NTRK1 (TRKA)2MAP2K1, MAP2K2
Signalling to ERKs2MAP2K1, MAP2K2
L1CAM interactions2MAP2K1, MAP2K2
Axon guidance2MAP2K1, MAP2K2
Signal transduction by L12MAP2K1, MAP2K2
Uptake and function of anthrax toxins2MAP2K1, MAP2K2
Uptake and actions of bacterial toxins2MAP2K1, MAP2K2
Diseases of signal transduction by growth factor receptors and second messengers2MAP2K1, MAP2K2
Infectious disease2MAP2K1, MAP2K2
RAF activation2MAP2K1, MAP2K2
RAF/MAP kinase cascade2MAP2K1, MAP2K2
MAP2K and MAPK activation2MAP2K1, MAP2K2
Negative feedback regulation of MAPK pathway2MAP2K1, MAP2K2
Negative regulation of MAPK pathway2MAP2K1, MAP2K2
MAPK family signaling cascades2MAP2K1, MAP2K2
MAPK1/MAPK3 signaling2MAP2K1, MAP2K2
Signaling by moderate kinase activity BRAF mutants2MAP2K1, MAP2K2
Signaling by high-kinase activity BRAF mutants2MAP2K1, MAP2K2
Signaling by RAS mutants2MAP2K1, MAP2K2
Signaling by BRAF and RAF1 fusions2MAP2K1, MAP2K2
Paradoxical activation of RAF signaling by kinase inactive BRAF2MAP2K1, MAP2K2
Oncogenic MAPK signaling2MAP2K1, MAP2K2
Signaling by Receptor Tyrosine Kinases2MAP2K1, MAP2K2

Dominant GO biological processes

GO termTargets
MAPK cascade2
heart development2
positive regulation of gene expression2
Schwann cell development2
thyroid gland development2
regulation of stress-activated MAPK cascade2
ERBB2-ERBB3 signaling pathway2
myelination2
positive regulation of DNA-templated transcription2
insulin-like growth factor receptor signaling pathway2
thymus development2
regulation of axon regeneration2
positive regulation of axonogenesis2
face development2
trachea formation2

Indications & clinical

Indications

52 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
thyroid gland papillary carcinoma3MONDO:0005075EFO:0000641
metastatic melanoma3MONDO:0005191EFO:0002617
soft tissue sarcoma3MONDO:0018078EFO:1001968
thyroid gland carcinoma3MONDO:0015075EFO:0002892
acute myeloid leukemia2MONDO:0018874EFO:0000222
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
metastatic prostate carcinoma2MONDO:0004956EFO:0000196
oral cavity neoplasm2MONDO:0021245EFO:0003868
hepatocellular carcinoma2MONDO:0007256EFO:0000182
thyroid gland follicular carcinoma2MONDO:0005034EFO:0000501
plasma cell myeloma2MONDO:0009693EFO:0001378
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
Erdheim-Chester disease2MONDO:0018153EFO:1000926
colorectal carcinoma2MONDO:0024331EFO:1001951
colorectal adenocarcinoma2MONDO:0005008EFO:0000365
breast neoplasm2MONDO:0021100MONDO:0007254
lung neoplasm2MONDO:0021117MONDO:0008903
epithelioid hemangioendothelioma2MONDO:0015523MONDO:0015523
ameloblastoma2MONDO:0017795MONDO:0017795
cholangiocarcinoma2MONDO:0019087EFO:0005221
undifferentiated carcinoma2MONDO:0005617EFO:0006772
histiocytosis2MONDO:0002637HP:0100727
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
colonic neoplasm2MONDO:0005401MONDO:0021063
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
craniopharyngioma2MONDO:0018907EFO:1000209
breast carcinoma2MONDO:0004989EFO:0000305
prostate carcinoma2MONDO:0005159EFO:0001663
biliary tract neoplasm2MONDO:0005304EFO:0003891
thyroid gland undifferentiated (anaplastic) carcinoma2MONDO:0006468EFO:1000595
uveal melanoma2MONDO:0006486EFO:1000616
colorectal neoplasm2MONDO:0005335MONDO:0005575
arteriovenous malformations of the brain2MONDO:0007154Orphanet:46724
leukemia1MONDO:0005059EFO:0000565
rectal cancer1MONDO:0006519EFO:1000657
lung adenocarcinoma1MONDO:0005061EFO:0000571
bronchial neoplasm1MONDO:0002807EFO:1000849
gastric neoplasm1MONDO:0021085MONDO:0001056
glioma1MONDO:0021042MONDO:0100342
amyotrophic lateral sclerosis1MONDO:0004976MONDO:0004976
meningioma1MONDO:0016642MONDO:0016642
rosacea1MONDO:0006604EFO:1000760
pancreatic ductal adenocarcinoma1MONDO:0005184MONDO:0005184

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

Clinical trials

Total trials: 251.

Phase distribution

PhaseTrials
PHASE2108
PHASE177
PHASE1/PHASE231
Not specified17
PHASE311
PHASE43
PHASE2/PHASE32
EARLY_PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03340506PHASE4RECRUITINGDabrafenib and/or Trametinib Rollover Study
NCT03975829PHASE4RECRUITINGPediatric Long-Term Follow-up and Rollover Study
NCT07010393PHASE4NOT_YET_RECRUITINGGenotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study
NCT02224781PHASE3ACTIVE_NOT_RECRUITINGDabrafenib and Trametinib Followed by Ipilimumab and Nivolumab or Ipilimumab and Nivolumab Followed by Dabrafenib and Trametinib in Treating Patients With Stage III-IV BRAFV600 Melanoma
NCT04940052PHASE3ACTIVE_NOT_RECRUITINGStudy of Efficacy and Safety of Dabrafenib in Combination With Trametinib in Previously Treated Patients With Metastatic, Radio-active Iodine Refractory BRAF V600E Mutation Positive Differentiated Thyroid Cancer
NCT06346067PHASE3ACTIVE_NOT_RECRUITINGA Study to Assess Naporafenib (ERAS-254) Administered With Trametinib in Patients With NRAS-mutant Melanoma (SEACRAFT-2)
NCT06475989PHASE3RECRUITINGStudy of Targeted Therapy vs. Chemotherapy in Patients With Thyroid Cancer
NCT07440290PHASE2/PHASE3NOT_YET_RECRUITINGDETERMINE Trial Treatment Arm 07: Dabrafenib in Combination With Trametinib in Adult, Paediatric and Teenage/Young Adult Patients With BRAF V600 Mutation-Positive Cancers.
NCT01245062PHASE3COMPLETEDGSK1120212 vs Chemotherapy in Advanced or Metastatic BRAF V600E/K Mutation-positive Melanoma
NCT01584648PHASE3COMPLETEDA Study Comparing Trametinib and Dabrafenib Combination Therapy to Dabrafenib Monotherapy in Subjects With BRAF-mutant Melanoma
NCT01597908PHASE3COMPLETEDDabrafenib Plus Trametinib vs Vemurafenib Alone in Unresectable or Metastatic BRAF V600E/K Cutaneous Melanoma
NCT01682083PHASE3COMPLETEDDabrafenib With Trametinib in the Adjuvant Treatment of High-risk BRAF V600 Mutation-positive Melanoma (COMBI-AD).
NCT02101788PHASE2/PHASE3COMPLETEDTrametinib in Treating Patients With Recurrent or Progressive Low-Grade Ovarian Cancer or Peritoneal Cavity Cancer
NCT02967692PHASE3TERMINATEDA Study of the Anti-PD1 Antibody PDR001, in Combination With Dabrafenib and Trametinib in Advanced Melanoma
NCT03551626PHASE3COMPLETEDStudy of Dabrafenib+Trametinib in the Adjuvant Treatment of Stage III BRAF V600+ Melanoma After Complete Resection to Evaluate the Impact on Pyrexia Related Outcomes
NCT03784014PHASE3COMPLETEDMolecular Profiling of Advanced Soft-tissue Sarcomas
NCT01972347PHASE2ACTIVE_NOT_RECRUITINGNeoadjuvant Dabrafenib + Trametinib for AJCC Stage IIIB-C BRAF V600 Mutation Positive Melanoma
NCT01979523PHASE2ACTIVE_NOT_RECRUITINGTrametinib With or Without GSK2141795 in Treating Patients With Metastatic Uveal Melanoma
NCT01989585PHASE1/PHASE2ACTIVE_NOT_RECRUITINGTesting the Addition of Navitoclax to the Combination of Dabrafenib and Trametinib in People Who Have BRAF Mutant Melanoma
NCT01990196PHASE2ACTIVE_NOT_RECRUITINGNeoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer
NCT02079740PHASE1/PHASE2ACTIVE_NOT_RECRUITINGTrametinib and Navitoclax in Treating Patients With Advanced or Metastatic Solid Tumors
NCT02152995PHASE2ACTIVE_NOT_RECRUITINGTrametinib in Increasing Tumoral Iodine Incorporation in Patients With Recurrent or Metastatic Thyroid Cancer
NCT02196181PHASE2ACTIVE_NOT_RECRUITINGTesting Two Different Treatment Schedules of Dabrafenib and Trametinib for Skin Cancer Which Has Spread
NCT02231775PHASE2ACTIVE_NOT_RECRUITINGDabrafenib and Trametinib Before and After Surgery in Treating Patients With Stage IIIB-C Melanoma With BRAF V600 Mutation
NCT02465060PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02642042PHASE2ACTIVE_NOT_RECRUITINGTrametinib and Docetaxel in Treating Patients With Recurrent or Stage IV KRAS Mutation Positive Non-small Cell Lung Cancer
NCT02881242PHASE2ACTIVE_NOT_RECRUITINGTrametinib in Treating Patients With Progressive Metastatic Hormone-Resistant Prostate Cancer
NCT02910700PHASE2ACTIVE_NOT_RECRUITINGNivolumab With Trametinib and Dabrafenib, or Encorafenib and Binimetinib in Treating Patients With BRAF Mutated Metastatic or Unresectable Stage III-IV Melanoma
NCT02925234PHASE2RECRUITINGThe Drug Rediscovery Protocol (DRUP Trial)
NCT03087071PHASE2ACTIVE_NOT_RECRUITINGPanitumumab With or Without Trametinib in Treating Patients With Stage IV Colorectal Cancer
NCT03149029PHASE2ACTIVE_NOT_RECRUITINGAbbreviated MAPK Targeted Therapy Plus Pembrolizumab in Melanoma
NCT03190915PHASE2ACTIVE_NOT_RECRUITINGTrametinib in Treating Patients With Relapsed or Refractory Juvenile Myelomonocytic Leukemia
NCT03225664PHASE1/PHASE2ACTIVE_NOT_RECRUITINGTrametinib and Pembrolizumab in Treating Patients With Recurrent Non-small Cell Lung Cancer That Is Metastatic, Unresectable, or Locally Advanced
NCT03363217PHASE2ACTIVE_NOT_RECRUITINGTrametinib for Pediatric Neuro-oncology Patients With Refractory Tumor and Activation of the MAPK/ERK Pathway.
NCT03563729PHASE2RECRUITINGMelanoma Metastasized to the Brain and Steroids
NCT03899155PHASE2RECRUITINGPan Tumor Rollover Study
NCT03919071PHASE2ACTIVE_NOT_RECRUITINGDabrafenib Combined With Trametinib After Radiation Therapy in Treating Patients With Newly-Diagnosed High-Grade Glioma
NCT04116541PHASE2RECRUITINGA Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors.
NCT04201457PHASE1/PHASE2ACTIVE_NOT_RECRUITINGA Trial of Dabrafenib, Trametinib and Hydroxychloroquine for Patients With Recurrent LGG or HGG With a BRAF Aberration
NCT04238624PHASE2ACTIVE_NOT_RECRUITINGStudy of Cemiplimab Combined With Dabrafenib and Trametinib in People With Anaplastic Thyroid Cancer

Clinical evidence (CIViC)

Variant × indication × effect (134 predictive associations from 144 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
BRAF V600EPleomorphic XanthoastrocytomaSensitivity/ResponseDabrafenib + TrametinibCIViC AEID11312 +1
BRAF V600Skin MelanomaSensitivity/ResponseDabrafenib + TrametinibCIViC AEID1411
BRAF V600EPilocytic AstrocytomaSensitivity/ResponseDabrafenib + TrametinibCIViC AEID11313
BRAF V600ESolid TumorSensitivity/ResponseTrametinib + DabrafenibCIViC AEID12161
BRAF V600ELow Grade GliomaSensitivity/ResponseDabrafenib + TrametinibCIViC AEID12162
BRAF V600ELung Non-small Cell CarcinomaSensitivity/ResponseDabrafenib + TrametinibCIViC AEID3017
BRAF V600EMelanomaSensitivity/ResponseTrametinibCIViC BEID2135 +2
BRAF V600KMelanomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID6939 +2
BRAF V600MelanomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID6180 +1
BRAF V600ECholangiocarcinomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID7453 +1
BRAF V600EMelanomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID6178 +1
BRAF V600EMelanomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID6938 +1
KRAS MutationLung Non-small Cell CarcinomaSensitivity/ResponseTrametinibCIViC BEID1220 +1
BRAF Non-V600Solid TumorSensitivity/ResponseTrametinibCIViC BEID7855
BRAF V600Colorectal CancerSensitivity/ResponseTrametinib + DabrafenibCIViC BEID1415
BRAF V600MelanomaSensitivity/ResponseTrametinibCIViC BEID1750
BRAF V600MelanomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID93
BRAF V600ECancerSensitivity/ResponseTrametinib + DabrafenibCIViC BEID11672
BRAF V600ESkin MelanomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID3758
BRAF V600EColorectal CancerSensitivity/ResponsePanitumumab + Dabrafenib + TrametinibCIViC BEID6123
BRAF V600EColorectal AdenocarcinomaSensitivity/ResponseTrametinib + PanitumumabCIViC BEID6124
BRAF V600EAnaplastic Thyroid CarcinomaSensitivity/ResponseDabrafenib + TrametinibCIViC BEID6975
BRAF V600EBiliary Tract CancerSensitivity/ResponseDabrafenib + TrametinibCIViC BEID7264
BRAF V600EOvarian CancerSensitivity/ResponseTrametinib + DabrafenibCIViC BEID7454
BRAF V600EPapillary Thyroid CarcinomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID7762
BRAF V600KMelanomaSensitivity/ResponseTrametinibCIViC BEID2506
BRAF V600KSkin MelanomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID4181
BRAF V600KMelanomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID6179
BRAF V600R AND BRAF Non-V600MelanomaSensitivity/ResponseTrametinib + DabrafenibCIViC BEID11308
GNAQ MutationUveal MelanomaSensitivity/ResponseTrametinibCIViC BEID1229

+104 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of CPIC Guideline for chlorpropamide, dabrafenib, gliclazidCPICG6PD

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.

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

MoleculeSourceStatusShared targets
BINIMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
COBIMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
FEDRATINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
RUXOLITINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
SELUMETINIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
SORAFENIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
VANDETANIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
VEMURAFENIBChEMBL + PubChemPhase 4 (approved)MAP2K1, MAP2K2
AXITINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
BOSUTINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
DASATINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
GILTERITINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
NERATINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
NINTEDANIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
SUNITINIBChEMBLPhase 4 (approved)MAP2K1, MAP2K2
AVUTOMETINIBChEMBLPhase 3MAP2K1, MAP2K2
CANERTINIBChEMBLPhase 3MAP2K1, MAP2K2
DOVITINIBChEMBLPhase 3MAP2K1, MAP2K2
LESTAURTINIBChEMBLPhase 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
AfatinibPubChemApprovedMAP2K1, MAP2K2
CrizotinibPubChemApprovedMAP2K1, MAP2K2
dacomitinibPubChemApprovedMAP2K1, MAP2K2
FostamatinibPubChemApprovedMAP2K1, MAP2K2
GefitinibPubChemApprovedMAP2K1, MAP2K2
IdelalisibPubChemApprovedMAP2K1, MAP2K2
PazopanibPubChemApprovedMAP2K1, MAP2K2
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
CapivasertibPubChemApprovedMAP2K2
CapmatinibPubChemApprovedMAP2K2
DabrafenibPubChemApprovedMAP2K2
EntrectinibPubChemApprovedMAP2K2
ErlotinibPubChemApprovedMAP2K2