Nilotinib

drug
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Also known as AMN 107AMN-107AMN107NSC-747599SID124894352SID99460838TasignaSID124894351NILOTINIB (AMN-107)Nilotinib hydrochloride monohydrateÊNilotinib hydrochloride monohydrateÂNilotinib

Summary

Nilotinib (CHEMBL255863) is an approved small-molecule antineoplastic agent (ATC L01EA03) targeting DDR1, DDR2, and ABL1; indicated across 27 conditions including neoplasm and chronic myeloid leukemia; with CIViC clinical evidence for 55 variant-indication associations (e.g. BCR::ABL1 Fusion in b-lymphoblastic leukemia/lymphoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EA03
  • Targets: 3 (DDR1, DDR2, ABL1)
  • Indications: 27 conditions
  • Clinical trials: 161
  • Precision-oncology evidence (CIViC): 55 variant–indication associations
  • Chemistry: 529.5 Da · C28H22F3N7O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL255863
NameNilotinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID644241
ChEBICHEBI:52172
ATCL01EA03
Molecular formulaC28H22F3N7O
Molecular weight529.5
InChIKeyHHZIURLSWUIHRB-UHFFFAOYSA-N

SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

IUPAC name: 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide

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

Also known as: AMN 107, AMN-107, AMN107, Nilotinib, NSC-747599, nilotinib, SID124894352, SID99460838, Tasigna, SID124894351, NILOTINIB, NILOTINIB (AMN-107)

Parent form; salt/anhydrous children: CHEMBL1201740, CHEMBL6068409

Patent coverage: 10,155 distinct patent families (38,627 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 38,522 (100%) 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
DDR1discoidin domain receptor tyrosine kinase 1Inhibition7.370.1%Q08345
DDR2discoidin domain receptor tyrosine kinase 2Inhibition9.30%Q16832
ABL1ABL proto-oncogene 1, non-receptor tyrosine kinaseInhibition7.81.2%P00519

Broader ChEMBL bioactivity targets: 90 (assay-derived). Sample: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, RAF proto-oncogene serine/threonine-protein kinase, Calcium-dependent protein kinase 1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Receptor-type tyrosine-protein kinase FLT3.

Bioactivity

ChEMBL activities: 222 potent at pChembl ≥ 5 of 228 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ABL19.48IC500.33nMCHEMBL_ACT_13280053
ABL19.06IC500.87nMCHEMBL_ACT_26276617
ABL19IC501nMCHEMBL_ACT_24707069
ABL18.96IC501.1nMCHEMBL_ACT_26276633
DDR18.96Kd1.1nMCHEMBL_ACT_7594531
ABL18.92IC501.2nMCHEMBL_ACT_20704576
DDR28.7IC502nMCHEMBL_ACT_14665982
ABL18.66IC502.2nMCHEMBL_ACT_26276621
ABL18.44Kd3.6nMCHEMBL_ACT_12617325
DDR18.43IC503.7nMCHEMBL_ACT_3471375
CA28.39Ki4.1nMCHEMBL_ACT_2692390
ABL18.31Kd4.9nMCHEMBL_ACT_18916459
ABL18.31Kd4.9nMCHEMBL_ACT_7594667
DDR28.28IC505.2nMCHEMBL_ACT_3471376
ABL18.26IC505.56nMCHEMBL_ACT_20609025
DDR28.22Kd6nMCHEMBL_ACT_14666022
DDR28.21Kd6.2nMCHEMBL_ACT_12617323
ABL18.15IC507nMCHEMBL_ACT_26325698
ABL18.05IC509nMCHEMBL_ACT_26325638
ABL18.05IC509nMCHEMBL_ACT_26325731
P005208IC5010nMCHEMBL_ACT_26325963
ABL18Kd10nMCHEMBL_ACT_7594670
ABL18Kd10nMCHEMBL_ACT_7594675
MAP3K207.96Kd11nMCHEMBL_ACT_7596380
ABL17.92IC5012nMCHEMBL_ACT_26325626
ABL17.92Kd12nMCHEMBL_ACT_7594665
ABL17.9IC5012.7nMCHEMBL_ACT_19289513
ABL17.89IC5012.8nMCHEMBL_ACT_12623337
ABL17.89IC5013nMCHEMBL_ACT_26325701
P005207.89IC5013nMCHEMBL_ACT_26325823

Target pathways

Aggregated over 3 target gene(s): DDR1, DDR2, ABL1.

Top Reactome pathways

54 total, by targets touching each:

PathwayTargetsGenes
Non-integrin membrane-ECM interactions2DDR1, DDR2
Hemostasis1ABL1
Developmental Biology1ABL1
Signal Transduction1ABL1
Cell Cycle1ABL1
Disease1ABL1
Innate Immune System1ABL1
Immune System1ABL1
Signaling by Rho GTPases1ABL1
RHO GTPase Effectors1ABL1
Fcgamma receptor (FCGR) dependent phagocytosis1ABL1
Regulation of actin dynamics for phagocytic cup formation1ABL1
Epigenetic regulation of gene expression1ABL1
Generic Transcription Pathway1ABL1
Signaling by ROBO receptors1ABL1
Axon guidance1ABL1
Role of ABL in ROBO-SLIT signaling1ABL1
Mitotic G1 phase and G1/S transition1ABL1
Myogenesis1ABL1
Infectious disease1ABL1
RHO GTPases Activate WASPs and WAVEs1ABL1
HDR through Single Strand Annealing (SSA)1ABL1
DNA Double-Strand Break Repair1ABL1
Homology Directed Repair1ABL1
Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks1ABL1
HDR through Homologous Recombination (HRR) or Single Strand Annealing (SSA)1ABL1
DNA Double Strand Break Response1ABL1
Cyclin D associated events in G11ABL1
G1 Phase1ABL1
Cell Cycle, Mitotic1ABL1

Dominant GO biological processes

GO termTargets
cell adhesion3
protein phosphorylation3
cell surface receptor protein tyrosine kinase signaling pathway2
regulation of extracellular matrix disassembly2
positive regulation of neuron projection development2
collagen-activated tyrosine kinase receptor signaling pathway2
protein autophosphorylation2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction2
positive regulation of fibroblast proliferation2
positive regulation of ERK1 and ERK2 cascade2
cellular response to transforming growth factor beta stimulus2
regulation of cell growth1
regulation of cell-matrix adhesion1
embryo implantation1
lactation1

Indications & clinical

Indications

27 indications (0 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
neoplasm3MONDO:0005070EFO:0000616
chronic myeloid leukemia3MONDO:0011996EFO:0000339
leukemia3MONDO:0005059EFO:0000565
soft tissue sarcoma3MONDO:0018078EFO:1001968
myeloid leukemia3MONDO:0004643MONDO:0004643
Alzheimer disease3MONDO:0004975MONDO:0004975
gastrointestinal stromal tumor3MONDO:0011719MONDO:0011719
acute lymphoblastic leukemia2MONDO:0004967EFO:0000220
acute myeloid leukemia2MONDO:0018874EFO:0000222
melanoma2MONDO:0005105EFO:0000756
pulmonary arterial hypertension2MONDO:0015924EFO:0001361
cutaneous melanoma2MONDO:0005012EFO:0000389
metastatic melanoma2MONDO:0005191EFO:0002617
cerebellar ataxia2MONDO:0000437MONDO:0000437
graft versus host disease2MONDO:0013730MONDO:0013730
Parkinson disease2MONDO:0005180MONDO:0005180
acoustic neuroma2MONDO:0001569HP:0009588
paraganglioma2MONDO:0000448EFO:1000453
glioma2MONDO:0021042MONDO:0021637
tenosynovial giant cell tumor, diffuse type2MONDO:0024686MONDO:0024686
breast neoplasm1MONDO:0021100MONDO:0007254
Huntington disease1MONDO:0007739MONDO:0007739
chordoma1MONDO:0008978MONDO:0008978
colonic neoplasm0MONDO:0005401MONDO:0021063

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

Clinical trials

Total trials: 161.

Phase distribution

PhaseTrials
PHASE260
PHASE127
PHASE326
Not specified18
PHASE417
PHASE1/PHASE210
EARLY_PHASE12
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04877522PHASE4RECRUITINGAsciminib Roll-over Study
NCT00756509PHASE4COMPLETEDTreatment of Patients With Metastatic or Unresectable Gastrointestinal Stromal Tumors in First Line With Nilotinib
NCT00786812PHASE4COMPLETEDStudy of Treatment With Nilotinib in Adult Patients With Imatinib - Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase
NCT00980018PHASE4COMPLETEDAn Exploratory Trial to Assess the Improvement of Adverse Events in Chronic Myelogenous Leukemia Patients Treated With Imatinib When Switched to Nilotinib Treatment
NCT01043874PHASE4COMPLETEDStudy to Evaluate Nilotinib in Chronic Myelogenous Leukemia (CML) Patients With SubOptimal Response
NCT01061177PHASE4COMPLETEDNilotinib in Newly Diagnosed Adult Philadelphia Chromosome & /or BCR-ABL Positive Chronic Myeloid Leukaemia in Chronic Phase
NCT01131325PHASE4TERMINATEDStudy of Nilotinib in Ph+ CML-CP Patients With Low Imatinib Trough Plasma Concentrations
NCT01206088PHASE4COMPLETEDTasigna in Glivec-resistant or Intolerant Patients in CML
NCT01227577PHASE4COMPLETEDCMR Rate of Newly Diagnosed CML-CP Patients Treated With Nilotinib
NCT01368523PHASE4COMPLETEDStudy of Oral AMN107 (Nilotinib) in Adult Patients With Imatinib - Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase Previously Enrolled to CAMN107A2109 Trial
NCT01605981PHASE4WITHDRAWNTrial Evaluating Nilotinib as Treatment for Newly Diagnosed CML Patients in Accelerated Phase.
NCT01735955PHASE4COMPLETEDStudy to Allow Access to Nilotinib for Patients Who Are on Nilotinib Treatment in a Novartis-sponsored Study
NCT02086487PHASE4TERMINATEDEfficacy and Safety Assessment of NIlotinib in CML Patients With Suboptimal Response on Imatinib Therapy
NCT02389920PHASE4UNKNOWNMulticenter, PhaseⅣ, Open Label Trial of Nilotinib in Adult Patients Diagnosed Philadelphia Chromosome Positive(Ph+) Chronic Myeloid Leukemia in CP/AP Intolerant to Dasatinib
NCT02546674PHASE4COMPLETEDStudy Assessing Deep Molecular Response in Adult Patients With CML in Chronic Phase Treated With Nilotinib Firstline.
NCT02602314PHASE4UNKNOWNSustained Treatment-free Remission in BCR-ABL+ Chronic Myeloid Leukemia
NCT03332511PHASE4COMPLETEDEfficacy and Safety of Nilotinib in CML-CP
NCT04971226PHASE3ACTIVE_NOT_RECRUITINGA Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
NCT05456191PHASE3ACTIVE_NOT_RECRUITINGA Study to Investigate Tolerability and Efficacy of Asciminib (Oral) Versus Nilotinib (Oral) in Adult Participants (≥18 Years of Age) With Newly Diagnosed Philadelphia Chromosome Positive Chronic Myelogenous Leukemia in Chronic Phase (Ph+ CML-CP)
NCT00264160PHASE2/PHASE3COMPLETEDEfficacy and Safety of Oral AMN107 in Adults With Chronic Myelogenous Leukemia Resistant and/or Intolerant to Imatinib Mesylate Therapy
NCT00471328PHASE3COMPLETEDEfficacy and Safety of Nilotinib (AMN107) Compared With Current Treatment Options in Patients With GIST Who Have Failed Both Imatinib and Sunitinib
NCT00471497PHASE3COMPLETEDA Study of Imatinib Versus Nilotinib in Adult Patients With Newly Diagnosed Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP)
NCT00519090PHASE3TERMINATEDNilotinib vs Imatinib in Adult Patients With Philadelphia (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP)
NCT00751036PHASE3TERMINATEDNilotinib 800 Mg And Imatinib 800 Mg For The Treatment Of Patients With Gastrointestinal Stromal Tumors (Gist) Refractory To Imatinib 400 Mg
NCT00760877PHASE3COMPLETEDNilotinib Versus Standard Imatinib (400/600 mg Every Day (QD)) Comparing the Kinetics of Complete Molecular Response for Chronic Myelogenous Leukemia in Chronic Phase (CML-CP) Pts With Evidence of Persistent Leukemia by Real-time Quantitative Polymerase Chain Reaction (RQ-PCR)
NCT00785785PHASE3COMPLETEDA Study of Nilotinib Versus Imatinib in GIST Patients
NCT00802841PHASE3COMPLETEDRandomized Phase Lll Study of Imatinib Dose Optimization vs Nilotinib in CML Patients With Suboptimal Response to Imatinib
NCT01126892PHASE3COMPLETEDA Study of Nilotinib in Adult Patients With Imatinib Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase
NCT01254188PHASE3COMPLETEDSafety and Efficacy of Nilotinib in Newly Diagnosed Chronic Myeloid Leukemia Patients
NCT01275196PHASE3COMPLETEDSafety and Efficacy of Nilotinib vs. Imatinib in the Treatment of Newly Diagnosed Chinese Ph+ CML-CP Patients
NCT01289028PHASE3COMPLETEDEfficacy of Nilotinib in Adult Patients With Gastrointestinal Stromal Tumors Resistant to Imatinib and Sunitinib.
NCT01400074PHASE3UNKNOWNEfficacy of Nilotinib Versus Imatinib in Ph+ CML in Early CP Who Have a Suboptimal Molecular Response to Imatinib
NCT01535391PHASE3COMPLETEDNilotinib in PH+, BCR-, ABL+ CML Patients
NCT01657604PHASE3COMPLETEDTKI and Interferon Alpha Evaluation Initiated by the German Chronic Myeloid Leukemia Study Group - the TIGER Study
NCT01743989PHASE3COMPLETEDA Randomized Phase III Study to Assess the Effect of a Longer Duration of Consolidation Treatment With Nilotinib on TFR in CP CML.
NCT01819389PHASE3COMPLETEDLow-dose Nilotinib and Imatinib Combination in Chronic Myeloid Leukemia Patients, With Failure, Suboptimal Response or Treatment Intolerance
NCT02108951PHASE3TERMINATEDStudy to Assess Efficacy and Safety of Nilotinib 300mg Twice Daily in Patients With Philadelphia Positive Chronic Myeloid Leukaemia (CML) in Chronic Phase Who Are Intolerant to Prior Tyrosine Kinase Inhibitors.
NCT02115386PHASE3TERMINATEDTrial to Evaluate the Improvement of Chronic Low-grade AEs in Patients With Ph+ CML With Optimal Response to Imatinib When Switched to Nilotinib
NCT02174445PHASE3TERMINATEDAn Open-label, Randomised Multicenter Phase 3b Study to Determine the Confirmed Rate of Molecular Response ≥ 4 Log (MR4) at Two Years
NCT02272777PHASE3COMPLETEDA Study of Imatinib and Nilotinib in Patients With Chronic Myelogenous Leukemia in Chronic Phase

Clinical evidence (CIViC)

Variant × indication × effect (55 predictive associations from 61 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
BCR::ABL1 FusionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponseNilotinibCIViC AEID11288
BCR::ABL1 FusionChronic Myeloid LeukemiaSensitivity/ResponseNilotinib + DasatinibCIViC AEID261
FLT3 MutationAcute Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC BEID5575 +1
ETV6::ABL1 FusionMyeloid NeoplasmSensitivity/ResponseImatinib + Dasatinib + NilotinibCIViC BEID11326
KIT MutationMelanomaSensitivity/ResponseNilotinibCIViC BEID7145
ABL1 TKD MutationChronic Myeloid LeukemiaResistanceNilotinibCIViC BEID6342
KIT AmplificationMelanomaResistanceNilotinibCIViC BEID5907
BCR::ABL1 Fusion AND ABL1 M244VChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC CEID2639
BCR::ABL1 Fusion AND ABL1 Y253HChronic Myeloid LeukemiaResistanceImatinib Mesylate + NilotinibCIViC CEID6200 +2
BCR::ABL1 Fusion AND ABL1 E255VChronic Myeloid LeukemiaResistanceImatinib Mesylate + NilotinibCIViC CEID6971 +1
BCR::ABL1 Fusion AND ABL1 E255KChronic Myeloid LeukemiaResistanceImatinib Mesylate + NilotinibCIViC CEID6232
BCR::ABL1 Fusion AND ABL1 F359CChronic Myeloid LeukemiaResistanceNilotinib + Imatinib MesylateCIViC CEID6233
BCR::ABL1 Fusion AND ABL1 F359VChronic Myeloid LeukemiaResistanceNilotinib + Imatinib MesylateCIViC CEID6970
ATF7IP::PDGFRB FusionChildhood B-cell Acute Lymphoblastic LeukemiaSensitivity/ResponseNilotinib + Imatinib + Dasatinib + Ponatinib + Bafetinib + RebastinibCIViC DEID7196
BCR::ABL1 FusionChronic Myeloid LeukemiaSensitivity/ResponseBafetinib + Nilotinib + DasatinibCIViC DEID7838
BCR::ABL1 Fusion AND ABL1 D276GChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC DEID2666
BCR::ABL1 Fusion AND ABL1 F486SChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC DEID2829
BCR::ABL1 Fusion AND ABL1 G398RChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC DEID2864
BCR::ABL1 Fusion AND ABL1 M351TChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC DEID2685
BCR::ABL1 Fusion AND ABL1 V299LChronic Myeloid LeukemiaSensitivity/ResponseNilotinibCIViC DEID2862
KIT L576PLung Non-small Cell CarcinomaSensitivity/ResponseImatinib + Dasatinib + NilotinibCIViC DEID303
KIT MutationAcute Promyelocytic LeukemiaSensitivity/ResponseNilotinibCIViC DEID5573
KIT V559DGastrointestinal Stromal TumorSensitivity/ResponseSorafenib + Nilotinib + Dasatinib + ImatinibCIViC DEID3033
NUP214::ABL1 FusionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponsePonatinib + Dasatinib + Imatinib + NilotinibCIViC DEID9150
BCR::ABL1 Fusion AND ABL1 F359CChronic Myeloid LeukemiaResistanceImatinib Mesylate + NilotinibCIViC DEID2854 +1
BCR::ABL1 Fusion AND ABL1 G250EChronic Myeloid LeukemiaResistanceNilotinibCIViC DEID2648 +1
BCR::ABL1 Fusion AND ABL1 E255KChronic Myeloid LeukemiaResistanceNilotinibCIViC DEID2662
BCR::ABL1 Fusion AND ABL1 E255KChronic Myeloid LeukemiaResistanceDasatinib + Nilotinib + Imatinib MesylateCIViC DEID6194
BCR::ABL1 Fusion AND ABL1 E255VChronic Myeloid LeukemiaResistanceNilotinibCIViC DEID2850
BCR::ABL1 Fusion AND ABL1 E292VChronic Myeloid LeukemiaResistanceNilotinibCIViC DEID2853

+25 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 13 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
AfatinibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
CABOZANTINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
DASATINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
ENTRECTINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
ERLOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
FEDRATINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
GefitinibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
IbrutinibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
LapatinibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
PONATINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
QUIZARTINIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
REGORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
RuxolitinibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
SORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
TirbanibulinChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
TOVORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
VANDETANIBChEMBL + PubChemPhase 4 (approved)ABL1, DDR1, DDR2
AXITINIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
BOSUTINIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
IMATINIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
LENVATINIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
NINTEDANIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
SUNITINIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
TIVOZANIBChEMBLPhase 4 (approved)ABL1, DDR1, DDR2
CEDIRANIBChEMBLPhase 3ABL1, DDR1, DDR2
DOVITINIBChEMBLPhase 3ABL1, DDR1, DDR2
LESTAURTINIBChEMBLPhase 3ABL1, DDR1, DDR2
LINIFANIBChEMBLPhase 3ABL1, DDR1, DDR2
MASITINIBChEMBLPhase 3ABL1, DDR1, DDR2
SARACATINIBChEMBLPhase 3ABL1, DDR1, DDR2
TESEVATINIBChEMBLPhase 3ABL1, DDR1, DDR2
AEE-788ChEMBLPhase 2ABL1, DDR1, DDR2
BAFETINIBChEMBLPhase 2ABL1, DDR1, DDR2
BMS-777607ChEMBLPhase 2ABL1, DDR1, DDR2
CEP-32496ChEMBLPhase 2ABL1, DDR1, DDR2
DANUSERTIBChEMBLPhase 2ABL1, DDR1, DDR2
DEFOSBARASERTIBChEMBLPhase 2ABL1, DDR1, DDR2
DORAMAPIMODChEMBLPhase 2ABL1, DDR1, DDR2
ENMD-2076ChEMBLPhase 2ABL1, DDR1, DDR2
FORETINIBChEMBLPhase 2ABL1, DDR1, DDR2
GLESATINIBChEMBLPhase 2ABL1, DDR1, DDR2
GOLVATINIBChEMBLPhase 2ABL1, DDR1, DDR2
MILCICLIBChEMBLPhase 2ABL1, DDR1, DDR2
OSI-632ChEMBLPhase 2ABL1, DDR1, DDR2
PEXMETINIBChEMBLPhase 2ABL1, DDR1, DDR2
R-406ChEMBLPhase 2ABL1, DDR1, DDR2
RAF-265ChEMBLPhase 2ABL1, DDR1, DDR2
REBASTINIBChEMBLPhase 2ABL1, DDR1, DDR2
TOZASERTIBChEMBLPhase 2ABL1, DDR1, DDR2
BinimetinibPubChemApprovedABL1, DDR1, DDR2
dacomitinibPubChemApprovedABL1, DDR1, DDR2
FostamatinibPubChemApprovedABL1, DDR1, DDR2
IdelalisibPubChemApprovedABL1, DDR1, DDR2
SelumetinibPubChemApprovedABL1, DDR1, DDR2
TrametinibPubChemApprovedABL1, DDR1, DDR2
DabrafenibChEMBL + PubChemPhase 4 (approved)ABL1, DDR1
MIDOSTAURINChEMBLPhase 4 (approved)ABL1, DDR1
BRIVANIBChEMBLPhase 3ABL1, DDR1