Regorafenib

drug
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Also known as BAY-734506BAY-734506 MONOHYDRATERegorafenib anhydrousRegorafenib hydrateRegorafenib monohydrateStivargaSID137275982

Summary

Regorafenib (CHEMBL1946170) is an approved small-molecule antineoplastic agent (ATC L01EX05) targeting KDR and BRAF; indicated across 41 conditions including colorectal adenocarcinoma and neoplasm; with CIViC clinical evidence for 50 variant-indication associations (e.g. KIT Exon 11 Mutation in gastrointestinal stromal tumor).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EX05
  • Targets: 2 (KDR, BRAF)
  • Indications: 41 conditions
  • Clinical trials: 241
  • Precision-oncology evidence (CIViC): 50 variant–indication associations
  • Chemistry: 482.8 Da · C21H15ClF4N4O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1946170
NameRegorafenib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11167602
ChEBICHEBI:68647
ATCL01EX05
Molecular formulaC21H15ClF4N4O3
Molecular weight482.8
InChIKeyFNHKPVJBJVTLMP-UHFFFAOYSA-N

SMILES: CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

IUPAC name: 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide

ChEBI definition: A pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previously received chemotherapy, anti-EGFR or anti-VEGF therapy.

Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, hepatotoxic agent.

Also known as: BAY-734506, BAY-734506 MONOHYDRATE, Regorafenib, Regorafenib anhydrous, Regorafenib hydrate, Regorafenib monohydrate, Stivarga, REGORAFENIB, SID137275982, regorafenib

Patent coverage: 5,357 distinct patent families (12,678 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 12,094 (95%) 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
KDRkinase insert domain receptorInhibition7.91.1%P35968
BRAFB-Raf proto-oncogene, serine/threonine kinaseInhibition7.558.6%P15056

Broader ChEMBL bioactivity targets: 50 (assay-derived). Sample: Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, RAF proto-oncogene serine/threonine-protein kinase, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Amine oxidase [flavin-containing] A, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Retinoic acid receptor gamma.

Bioactivity

ChEMBL activities: 117 potent at pChembl ≥ 5 of 122 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
EPHX29.3IC500.5nMCHEMBL_ACT_13349258
BRAF8.82IC501.5nMCHEMBL_ACT_19239343
TEK8.82IC501.5nMCHEMBL_ACT_19239344
P359178.82IC501.5nMCHEMBL_ACT_19239345
P359188.82IC501.5nMCHEMBL_ACT_19239346
FLT18.82IC501.5nMCHEMBL_ACT_19239347
PDGFRB8.82IC501.5nMCHEMBL_ACT_19239348
RAF18.82IC501.5nMCHEMBL_ACT_19239349
FGFR18.82IC501.5nMCHEMBL_ACT_19239350
RET8.82IC501.5nMCHEMBL_ACT_24867135
RET8.82IC501.5nMCHEMBL_ACT_24906930
RET8.82IC501.5nMCHEMBL_ACT_25871811
RET8.82IC501.5nMCHEMBL_ACT_26137494
RAF18.6IC502.5nMCHEMBL_ACT_24867133
RAF18.6IC502.5nMCHEMBL_ACT_25871810
RAF18.6IC502.5nMCHEMBL_ACT_26137495
RAF18.6IC502.5nMCHEMBL_ACT_29065624
KDR8.4IC504nMCHEMBL_ACT_24788770
KDR8.38IC504.2nMCHEMBL_ACT_18854163
KDR8.38IC504.2nMCHEMBL_ACT_19449716
KDR8.38IC504.2nMCHEMBL_ACT_24867138
KDR8.38IC504.2nMCHEMBL_ACT_25663322
P359188.38IC504.2nMCHEMBL_ACT_25871806
KDR8.38IC504.2nMCHEMBL_ACT_26001069
P359188.38IC504.2nMCHEMBL_ACT_26137490
KDR8.38Ki4.2nMCHEMBL_ACT_27790676
KDR8.38IC504.2nMCHEMBL_ACT_29065620
PDGFRA8.38IC504.2nMCHEMBL_ACT_29279127
KDR8.34IC504.6nMCHEMBL_ACT_25484193
KDR8.3IC505nMCHEMBL_ACT_19238842

Target pathways

Aggregated over 2 target gene(s): KDR, BRAF.

Top Reactome pathways

46 total, by targets touching each:

PathwayTargetsGenes
Spry regulation of FGF signaling1BRAF
Signal Transduction1BRAF
Disease1BRAF
Signaling by NTRKs1BRAF
Prolonged ERK activation events1BRAF
Frs2-mediated activation1BRAF
ARMS-mediated activation1BRAF
Signaling by NTRK1 (TRKA)1BRAF
Signalling to ERKs1BRAF
Signalling to p38 via RIT and RIN1BRAF
Signaling by FGFR1BRAF
Neuropilin interactions with VEGF and VEGFR1KDR
VEGF binds to VEGFR leading to receptor dimerization1KDR
Integrin cell surface interactions1KDR
VEGFA-VEGFR2 Pathway1KDR
VEGFR2 mediated cell proliferation1KDR
Negative regulation of FGFR1 signaling1BRAF
Negative regulation of FGFR2 signaling1BRAF
Negative regulation of FGFR3 signaling1BRAF
Negative regulation of FGFR4 signaling1BRAF
Signaling by FGFR11BRAF
Signaling by FGFR21BRAF
Signaling by FGFR31BRAF
Signaling by FGFR41BRAF
Diseases of signal transduction by growth factor receptors and second messengers1BRAF
RAF activation1BRAF
RAF/MAP kinase cascade1BRAF
MAP2K and MAPK activation1BRAF
Negative feedback regulation of MAPK pathway1BRAF
Negative regulation of MAPK pathway1BRAF

Dominant GO biological processes

GO termTargets
negative regulation of neuron apoptotic process2
positive regulation of ERK1 and ERK2 cascade2
negative regulation of endothelial cell apoptotic process2
protein phosphorylation2
cell differentiation2
negative regulation of apoptotic process2
angiogenesis1
ovarian follicle development1
branching involved in blood vessel morphogenesis1
vasculogenesis1
positive regulation of protein phosphorylation1
positive regulation of endothelial cell proliferation1
lymph vessel development1
positive regulation of mesenchymal cell proliferation1
epithelial cell maturation1

Indications & clinical

Indications

41 indications (6 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
colorectal adenocarcinoma4MONDO:0005008EFO:0000365
neoplasm4MONDO:0005070EFO:0000616
colorectal neoplasm4MONDO:0005335EFO:0004142
colorectal carcinoma4MONDO:0024331EFO:1001951
hepatocellular carcinoma3MONDO:0007256EFO:0000182
colonic neoplasm3MONDO:0005401MONDO:0021063
gastrointestinal stromal tumor3MONDO:0011719MONDO:0011719
adenoid cystic carcinoma2MONDO:0004971EFO:0000231
bile duct carcinoma2MONDO:0005496EFO:0005540
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
sarcoma2MONDO:0005089EFO:0000691
cholangiocarcinoma2MONDO:0019087EFO:0005221
ovarian neoplasm2MONDO:0021068EFO:0003893
melanoma2MONDO:0005105EFO:0000756
ovarian carcinoma2MONDO:0005140EFO:0001075
rectal cancer2MONDO:0006519EFO:1000657
glioblastoma2MONDO:0018177EFO:0000519
liposarcoma2MONDO:0005060EFO:0000569
osteosarcoma2MONDO:0009807EFO:0000637
renal cell carcinoma2MONDO:0005086EFO:0000681
angiosarcoma2MONDO:0016982EFO:0003968
cutaneous melanoma2MONDO:0005012EFO:0000389
macular degeneration2MONDO:0003004EFO:0009606
colon adenocarcinoma2MONDO:0002271EFO:1001949
soft tissue sarcoma2MONDO:0018078EFO:1001968
gastric neoplasm2MONDO:0021085MONDO:0001056
fallopian tube neoplasm2MONDO:0021092MONDO:0002158
ovarian cancer2MONDO:0008170MONDO:0008170
intrahepatic cholangiocarcinoma2MONDO:0003210EFO:1001961
meningioma2MONDO:0016642MONDO:0020634
acute myeloid leukemia1MONDO:0018874EFO:0000222
small cell lung carcinoma1MONDO:0008433EFO:0000702
rhabdomyosarcoma1MONDO:0005212EFO:0002918
bone cancer1MONDO:0002129EFO:1000350
myelodysplastic syndrome1MONDO:0018881EFO:0000198

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

Clinical trials

Total trials: 241.

Phase distribution

PhaseTrials
PHASE2129
PHASE132
PHASE1/PHASE228
Not specified23
PHASE321
PHASE2/PHASE37
PHASE41

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04874207PHASE4COMPLETEDEvaluation of Treatment PERSOnalization Based on Its Therapeutic Monitoring in Patients With Metastatic Colorectal Cancer Treated With REgorafenib
NCT03829462PHASE3ACTIVE_NOT_RECRUITINGAssessing a Regorafenib-irinotecan Combination Versus Regorafenib Alone in Metastatic Colorectal Cancer Patients
NCT03970447PHASE2/PHASE3RECRUITINGA Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma
NCT04879368PHASE3ACTIVE_NOT_RECRUITINGRegoNivo vs Standard of Care Chemotherapy in AGOC
NCT05425940PHASE3ACTIVE_NOT_RECRUITINGStudy of XL092 + Atezolizumab vs Regorafenib in Participants With Metastatic Colorectal Cancer
NCT05462613PHASE2/PHASE3RECRUITINGRegorafenib With Low-dose Chemotherapies and Aspirin Followed by Standard Chemotherapies in Metastatic Colorectal Cancer
NCT05794971PHASE3RECRUITINGRegorafenib Combined With Irinotecan Drug-Eluting Beads for Colorectal Cancer Liver Metastases
NCT06199973PHASE3ACTIVE_NOT_RECRUITINGInjection of SHR-A1811 Versus Physician Choiced Treatment in Patients With Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-fu, and Irinotecan
NCT06820957PHASE2/PHASE3ACTIVE_NOT_RECRUITINGTesting a New Combination of Anti-cancer Drugs in Patients Newly Diagnosed With Ewing Sarcoma Who Have Cancer That Has Spread to Other Parts of the Body
NCT07134205PHASE3NOT_YET_RECRUITINGThe Study of JMT101 Combined With Irinotecan as a ≥3rd-Line Treatment in Metastatic Colorectal Cancer
NCT07300488PHASE2/PHASE3ACTIVE_NOT_RECRUITINGEfficacy and Safety of Pracytarabine Versus Regorafenib in the Treatment of Patients With Hepatocellular Carcinoma
NCT07379047PHASE2/PHASE3NOT_YET_RECRUITINGEfficacy and Safety of NB003 in Patients With Advanced Gastrointestinal Stromal Tumors (GIST)
NCT07384377PHASE3NOT_YET_RECRUITINGJSKN003 Versus Physician Choiced Treatment in Patients With HER2-positive and Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-Fu, and Irinotecan
NCT07392866PHASE2/PHASE3NOT_YET_RECRUITINGA Clinical Study of SH006 Injection in Combination Therapy Versus Regorafenib in the Treatment of Advanced Hepatocellular Carcinoma
NCT07483684PHASE3NOT_YET_RECRUITINGA Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs
NCT01189903PHASE2/PHASE3UNKNOWNClinical Evaluation - A Phase IIA Proof of Concept Study of Regorafenib (Bayer 73-4506) in Biopsy-amenable Asian Colorectal Cancer Patients
NCT01584830PHASE3COMPLETEDAsian Subjects With Metastatic Colorectal Cancer Treated With Regorafenib or Placebo After Failure of Standard Therapy
NCT01786538PHASE3WITHDRAWNSecond-line FOLFOX With or Without Regorafenib in mCRC Patients Failed to First-line Irinotecan Plus Fluoropyrimidines
NCT02664077PHASE3TERMINATEDA Study Evaluating Regorafenib Following Completion of Standard Chemotherapy for Patients With Colon Cancer
NCT02773524PHASE3UNKNOWNA Study of Regorafenib in Refractory Advanced Gastro-Oesophageal Cancer
NCT02788279PHASE3COMPLETEDA Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma (COTEZO IMblaze370)
NCT02934529PHASE3COMPLETEDMetastatic Colorectal Cancer (RAS-wildtype) After Response to First-line Treatment With FOLFIR Plus Cetuximab
NCT03465722PHASE3COMPLETED(VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST
NCT04776148PHASE3COMPLETEDStudy of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017)
NCT04985136PHASE3TERMINATEDA Study of Camrelizumab Combined With Rivoceranib Mesylate Versus Investigator’s Choice of Regimen in Treatment of Patients With Advanced Hepatocellular Carcinoma (HCC)
NCT05064059PHASE3COMPLETEDA Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)
NCT05198934PHASE3COMPLETEDSotorasib and Panitumumab Versus Investigator’s Choice for Participants With Kirsten Rat Sarcoma (KRAS) p.G12C Mutation
NCT05328908PHASE3TERMINATEDA Study of Nivolumab-relatlimab Fixed-dose Combination Versus Regorafenib or TAS-102 in Participants With Later-lines of Metastatic Colorectal Cancer
NCT05600309PHASE3COMPLETEDA Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)-China Extension Study
NCT02389244PHASE2ACTIVE_NOT_RECRUITINGA Phase II Study Evaluating Efficacy and Safety of Regorafenib in Patients With Metastatic Bone Sarcomas
NCT02657551PHASE2ACTIVE_NOT_RECRUITINGA Study Using Regorafenib as Second or Third Line Therapy in Metastatic Medullary Thyroid Cancer
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
NCT02925234PHASE2RECRUITINGThe Drug Rediscovery Protocol (DRUP Trial)
NCT02955940PHASE2ACTIVE_NOT_RECRUITINGAn Open-Label Study to Enable Continued Treatment Access for Subjects Previously Enrolled in Studies of Ruxolitinib
NCT03657641PHASE1/PHASE2ACTIVE_NOT_RECRUITINGRegorafenib and Pembrolizumab in Treating Participants With Advanced or Metastatic Colorectal Cancer
NCT03844620PHASE2ACTIVE_NOT_RECRUITINGCirculating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer
NCT03899428PHASE2RECRUITINGImmune Checkpoint Therapy vs Target Therapy in Reducing Serum HBsAg Levels in Patients With HBsAg+ Advanced Stage HCC
NCT04116541PHASE2RECRUITINGA Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors.
NCT04117945PHASE2ACTIVE_NOT_RECRUITINGRegorafenib, With Cetuximab or Panitumumab, for the Treatment of Unresectable, Locally Advanced, or Metastatic Colorectal Cancer
NCT04625907PHASE1/PHASE2RECRUITINGFaR-RMS: An Overarching Study for Children and Adults With Frontline and Relapsed RhabdoMyoSarcoma

Clinical evidence (CIViC)

Variant × indication × effect (50 predictive associations from 54 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
KIT Exon 11 MutationGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC BEID4599 +2
KIT Exon 9 MutationGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC BEID4628
KIT WildtypeGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC BEID4144
KRAS Exon 2 MutationColorectal CancerSensitivity/ResponseRegorafenib AnhydrousCIViC BEID87
KIT Exon 9 MutationGastrointestinal Stromal TumorReduced SensitivityRegorafenib AnhydrousCIViC BEID4139 +1
PIK3CA E542KColorectal CancerResistanceRegorafenib AnhydrousCIViC BEID83
BRAF Exon 15 MutationGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC CEID4121
BRAF Kinase Domain DuplicationAcinic Cell CarcinomaSensitivity/ResponseRegorafenibCIViC CEID12470
FLT3 AmplificationColorectal CancerSensitivity/ResponseRegorafenib AnhydrousCIViC CEID7102
KDR R961WColorectal AdenocarcinomaSensitivity/ResponseRegorafenib AnhydrousCIViC CEID1191
KIT D820YGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC CEID4589
KIT N822KGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC CEID4595
KRAS G12ALung Non-small Cell CarcinomaSensitivity/ResponseRegorafenib AnhydrousCIViC CEID3716
KRAS G12DColorectal CancerResistanceRegorafenib AnhydrousCIViC CEID3947 +1
BRAF Exon 15 MutationGastrointestinal Stromal TumorResistanceRegorafenib AnhydrousCIViC CEID4605
BRAF V600EColon CancerSensitivity/ResponseRegorafenib AnhydrousCIViC DEID3776
KIT A502_Y503dupCancerSensitivity/ResponseImatinib + Ponatinib + Regorafenib AnhydrousCIViC DEID4630
KIT K550_W557delGastrointestinal Stromal TumorSensitivity/ResponseSunitinib + Imatinib + Regorafenib Anhydrous + PonatinibCIViC DEID4583
KIT K558delinsNPGastrointestinal Stromal TumorSensitivity/ResponseSunitinib + Ponatinib + Regorafenib Anhydrous + ImatinibCIViC DEID4594
KIT K642EGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC DEID4146
KIT P551_E554delPMYEGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib Anhydrous + Sunitinib + ImatinibCIViC DEID4455
KIT V559DGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib Anhydrous + Ponatinib + ImatinibCIViC DEID4459
KIT V560DGastrointestinal Stromal TumorSensitivity/ResponseSunitinib + Ponatinib + Regorafenib Anhydrous + ImatinibCIViC DEID4127
KIT V560GGastrointestinal Stromal TumorSensitivity/ResponseImatinib + Ponatinib + Regorafenib AnhydrousCIViC DEID7395
KIT V560_L576delGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC DEID4061
KIT W557_K558delGastrointestinal Stromal TumorSensitivity/ResponseSunitinib + Regorafenib AnhydrousCIViC DEID4087
KRAS G12VColon CancerSensitivity/ResponseRegorafenib AnhydrousCIViC DEID3932
KRAS G13DColon CancerSensitivity/ResponseRegorafenib AnhydrousCIViC DEID3897
RET C634WGastrointestinal Stromal TumorSensitivity/ResponseRegorafenib AnhydrousCIViC DEID3695
FBXW7 G579WColorectal CancerResistanceRegorafenib AnhydrousCIViC DEID4822

+20 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

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

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)BRAF, KDR
GEFITINIBChEMBL + PubChemPhase 4 (approved)BRAF, KDR
PAZOPANIBChEMBL + PubChemPhase 4 (approved)BRAF, KDR
ABEMACICLIBChEMBLPhase 4 (approved)BRAF, KDR
DASATINIBChEMBLPhase 4 (approved)BRAF, KDR
ERLOTINIBChEMBLPhase 4 (approved)BRAF, KDR
FEDRATINIBChEMBLPhase 4 (approved)BRAF, KDR
IMATINIBChEMBLPhase 4 (approved)BRAF, KDR
INFIGRATINIBChEMBLPhase 4 (approved)BRAF, KDR
PONATINIBChEMBLPhase 4 (approved)BRAF, KDR
SORAFENIBChEMBLPhase 4 (approved)BRAF, KDR
VEMURAFENIBChEMBLPhase 4 (approved)BRAF, KDR
MOTESANIBChEMBLPhase 3BRAF, KDR
QUERCETINChEMBLPhase 3BRAF, KDR
CEP-32496ChEMBLPhase 2BRAF, KDR
DORAMAPIMODChEMBLPhase 2BRAF, KDR
ELLAGIC ACIDChEMBLPhase 2BRAF, KDR
FORETINIBChEMBLPhase 2BRAF, KDR
R-406ChEMBLPhase 2BRAF, KDR
RAF-265ChEMBLPhase 2BRAF, KDR
REBASTINIBChEMBLPhase 2BRAF, KDR
AfatinibPubChemApprovedBRAF, KDR
BinimetinibPubChemApprovedBRAF, KDR
SelumetinibPubChemApprovedBRAF, KDR
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)KDR
ABROCITINIBChEMBLPhase 4 (approved)KDR
ACALABRUTINIBChEMBLPhase 4 (approved)KDR
ALECTINIBChEMBLPhase 4 (approved)KDR
AUROTHIOGLUCOSEChEMBLPhase 4 (approved)KDR
AXITINIBChEMBLPhase 4 (approved)KDR
BRIGATINIBChEMBLPhase 4 (approved)KDR
CABOZANTINIBChEMBLPhase 4 (approved)KDR
CABOZANTINIB S-MALATEChEMBLPhase 4 (approved)KDR
CERITINIBChEMBLPhase 4 (approved)KDR
COBIMETINIBChEMBLPhase 4 (approved)BRAF
DABRAFENIBChEMBLPhase 4 (approved)BRAF
ENASIDENIBChEMBLPhase 4 (approved)KDR
ENCORAFENIBChEMBLPhase 4 (approved)BRAF
ENTRECTINIBChEMBLPhase 4 (approved)KDR
ERDAFITINIBChEMBLPhase 4 (approved)KDR
ESTRAMUSTINEChEMBLPhase 4 (approved)KDR
FOSTAMATINIB DISODIUMChEMBLPhase 4 (approved)KDR
FRUQUINTINIBChEMBLPhase 4 (approved)KDR
FUTIBATINIBChEMBLPhase 4 (approved)KDR
GLAFENINEChEMBLPhase 4 (approved)KDR
HEXACHLOROPHENEChEMBLPhase 4 (approved)KDR
IBRUTINIBChEMBLPhase 4 (approved)KDR
INDIGOTINDISULFONATEChEMBLPhase 4 (approved)KDR
ISOXICAMChEMBLPhase 4 (approved)KDR
LENVATINIBChEMBLPhase 4 (approved)KDR
MEBENDAZOLEChEMBLPhase 4 (approved)KDR
MESALAMINEChEMBLPhase 4 (approved)KDR
MIDOSTAURINChEMBLPhase 4 (approved)KDR
NERATINIBChEMBLPhase 4 (approved)KDR
NICLOSAMIDEChEMBLPhase 4 (approved)KDR
NILOTINIBChEMBLPhase 4 (approved)BRAF
NINTEDANIBChEMBLPhase 4 (approved)KDR
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)KDR
NOVOBIOCINChEMBLPhase 4 (approved)KDR
OLMUTINIBChEMBLPhase 4 (approved)KDR