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Dasatinib Anhydrous

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Also known as BMS-354825Dasatinib (anhydrous)Dasatinib accordDasatinib accordpharmaDasatinibSprycel

Summary

Dasatinib Anhydrous (CHEMBL1421) is an approved small-molecule antineoplastic agent (ATC L01EA02) targeting ABL1, SIK1, and SIK2; indicated across 87 conditions including chronic myeloid leukemia and acute lymphoblastic leukemia; with CIViC clinical evidence for 223 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: L01EA02
  • Targets: 5 (ABL1, SIK1, SIK2…)
  • Indications: 87 conditions
  • Clinical trials: 316
  • Precision-oncology evidence (CIViC): 223 variant–indication associations
  • Chemistry: 488 Da · C22H26ClN7O2S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1421
NameDasatinib Anhydrous
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3062316
ChEBICHEBI:49375
ATCL01EA02
Molecular formulaC22H26ClN7O2S
Molecular weight488
InChIKeyZBNZXTGUTAYRHI-UHFFFAOYSA-N

SMILES: CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO

IUPAC name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide

ChEBI definition: An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name ‘dasatinib’ is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).

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

Also known as: BMS-354825, Dasatinib (anhydrous), Dasatinib accord, Dasatinib accordpharma, Dasatinib anhydrous, DASATINIB ANHYDROUS, Dasatinib, Sprycel, DASATINIB

Parent form; salt/anhydrous children: CHEMBL5314601, CHEMBL5416410

Patent coverage: 14,539 distinct patent families (55,003 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 54,779 (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
ABL1ABL proto-oncogene 1, non-receptor tyrosine kinaseInhibition10.491.2%P00519
SIK1salt inducible kinase 1Inhibition8.521%P57059
SIK2salt inducible kinase 2Inhibition8.520.5%Q9H0K1
SIK3SIK family kinase 3Inhibition81.3%Q9Y2K2
SRCSRC proto-oncogene, non-receptor tyrosine kinaseInhibition9.13.7%P12931

Broader ChEMBL bioactivity targets: 33 (assay-derived). Sample: Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Mast/stem cell growth factor receptor Kit, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Ephrin type-A receptor 2, Tyrosine-protein kinase Yes, Bcr/Abl fusion protein, Myelin transcription factor 1.

Bioactivity

ChEMBL activities: 129 potent at pChembl ≥ 5 of 129 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ABL110IC500.1nMCHEMBL_ACT_26325627
ABL19.7IC500.2nMCHEMBL_ACT_26325612
EPHA39.52IC500.3nMCHEMBL_ACT_26216933
ABL19.52IC500.3nMCHEMBL_ACT_26325600
ABL19.4IC500.4nMCHEMBL_ACT_26325606
ABL19.3IC500.5nMCHEMBL_ACT_26276632
ABL19.3IC500.5nMCHEMBL_ACT_26325630
ABL19.3IC500.5nMCHEMBL_ACT_26325636
ABL19.3IC500.5nMCHEMBL_ACT_26325639
ABL19.3IC500.5nMCHEMBL_ACT_26325723
ABL19.22IC500.6nMCHEMBL_ACT_26325594
ABL19.22IC500.6nMCHEMBL_ACT_26325615
ABL19.15IC500.7nMCHEMBL_ACT_26276620
ABL19.15IC500.7nMCHEMBL_ACT_26325633
ABL19.1IC500.8nMCHEMBL_ACT_26325597
ABL19.1IC500.8nMCHEMBL_ACT_26325642
SRC9.1IC500.8nMCHEMBL_ACT_26325645
ABL19.1IC500.8nMCHEMBL_ACT_26325699
P005209.1IC500.8nMCHEMBL_ACT_26325824
SRC9.1IC500.8nMCHEMBL_ACT_29127162
ABL19.05IC500.9nMCHEMBL_ACT_26325618
ABL19.05IC500.9nMCHEMBL_ACT_26325624
ABL19.05IC500.9nMCHEMBL_ACT_26325702
ABL19IC501nMCHEMBL_ACT_26276828
ABL18.96IC501.1nMCHEMBL_ACT_26276616
ABL18.96IC501.1nMCHEMBL_ACT_26276825
ABL18.94IC501.15nMCHEMBL_ACT_26325729
EPHA88.89IC501.3nMCHEMBL_ACT_26216948
ABL18.85IC501.4nMCHEMBL_ACT_26325714
ABL18.82IC501.5nMCHEMBL_ACT_26325717

Target pathways

Aggregated over 5 target gene(s): ABL1, SIK1, SIK2, SIK3, SRC.

Top Reactome pathways

156 total, by targets touching each:

PathwayTargetsGenes
Hemostasis2ABL1, SRC
Developmental Biology2ABL1, SRC
Signal Transduction2ABL1, SRC
Disease2ABL1, SRC
Immune System2ABL1, SRC
Signaling by Rho GTPases2ABL1, SRC
Generic Transcription Pathway2ABL1, SRC
Signaling by ROBO receptors2ABL1, SRC
Axon guidance2ABL1, SRC
Infectious disease2ABL1, SRC
Cyclin D associated events in G12ABL1, SRC
RNA Polymerase II Transcription2ABL1, SRC
Gene expression (Transcription)2ABL1, SRC
Transcriptional regulation by RUNX22ABL1, SRC
Transcriptional regulation by RUNX12ABL1, SRC
RUNX2 regulates osteoblast differentiation2ABL1, SRC
RUNX2 regulates bone development2ABL1, SRC
FCGR3A-mediated phagocytosis2ABL1, SRC
Nervous system development2ABL1, SRC
Signaling by Rho GTPases, Miro GTPases and RHOBTB32ABL1, SRC
Neurotransmitter receptors and postsynaptic signal transmission1SRC
Transmission across Chemical Synapses1SRC
Neuronal System1SRC
Signaling by ERBB21SRC
Signaling by ERBB41SRC
Nuclear signaling by ERBB41SRC
Downregulation of ERBB4 signaling1SRC
PIP3 activates AKT signaling1SRC
Cytokine Signaling in Immune system1SRC
Spry regulation of FGF signaling1SRC

Dominant GO biological processes

GO termTargets
intracellular signal transduction5
protein phosphorylation5
protein autophosphorylation3
epidermal growth factor receptor signaling pathway2
integrin-mediated signaling pathway2
substrate adhesion-dependent cell spreading2
Fc-gamma receptor signaling pathway involved in phagocytosis2
ephrin receptor signaling pathway2
cellular response to hydrogen peroxide2
positive regulation of ERK1 and ERK2 cascade2
cellular response to transforming growth factor beta stimulus2
cell adhesion2
regulation of cell differentiation2
negative regulation of transcription by RNA polymerase II2
cell differentiation2

Indications & clinical

Indications

87 indications (9 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
chronic myeloid leukemia4MONDO:0011996EFO:0000339
acute lymphoblastic leukemia4MONDO:0004967EFO:0000220
neoplasm4MONDO:0005070EFO:0000616
lymphoid leukemia4MONDO:0005402EFO:0004289
childhood malignant neoplasm4MONDO:0006517EFO:1000654
blast phase chronic myelogenous leukemia, BCR-ABL1 positive4MONDO:0006115EFO:1000131
leukemia3MONDO:0005059EFO:0000565
acute myeloid leukemia3MONDO:0018874EFO:0000222
prostate adenocarcinoma3MONDO:0005082EFO:0000673
metastatic prostate carcinoma3MONDO:0004956EFO:0000196
B-cell chronic lymphocytic leukemia2MONDO:0004948EFO:0000095
plasma cell myeloma2MONDO:0009693EFO:0001378
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
glioblastoma2MONDO:0018177EFO:0000519
metastatic melanoma2MONDO:0005191EFO:0002617
malignant pleural mesothelioma2MONDO:0005112EFO:0000770
diffuse large B-cell lymphoma2MONDO:0018905EFO:0000403
melanoma2MONDO:0005105EFO:0000756
mesothelioma2MONDO:0005065EFO:0000588
acquired polycythemia vera2MONDO:0009891EFO:0002429
breast neoplasm2MONDO:0021100EFO:0003869
lymphoma2MONDO:0005062EFO:0000574
small cell lung carcinoma2MONDO:0008433EFO:0000702
cholangiocarcinoma2MONDO:0019087EFO:0005221
chronic kidney disease2MONDO:0005300EFO:0003884
gliosarcoma2MONDO:0016681EFO:1001465
head and neck squamous cell carcinoma2MONDO:0010150EFO:0000181
cutaneous melanoma2MONDO:0005012EFO:0000389
neuroblastoma2MONDO:0005072EFO:0000621
pineoblastoma2MONDO:0016722EFO:1000475
brain neoplasm2MONDO:0021211EFO:0003833
diffuse intrinsic pontine glioma2MONDO:0006033EFO:1000026
rectal cancer2MONDO:0006519EFO:1000657
adenoid cystic carcinoma2MONDO:0004971MONDO:0003175
lung neoplasm2MONDO:0021117MONDO:0008903
colonic neoplasm2MONDO:0005401MONDO:0021063
glioma2MONDO:0021042MONDO:0100342
brain disorder2MONDO:0005560EFO:0005774
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
breast carcinoma2MONDO:0004989EFO:0000305
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
HIV infectious disease2MONDO:0005109EFO:0000180
squamous cell carcinoma2MONDO:0005096EFO:0000707
obesity disorder2MONDO:0011122EFO:0001073
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
paraganglioma2MONDO:0000448EFO:1000453
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
Hodgkins lymphoma1MONDO:0004952EFO:0000183
MALT lymphoma1MONDO:0007650EFO:0000191
myelodysplastic syndrome1MONDO:0018881EFO:0000198
angioimmunoblastic T-cell lymphoma1MONDO:0004977EFO:0000255
Burkitt lymphoma1MONDO:0007243EFO:0000309
idiopathic pulmonary fibrosis1MONDO:0800504EFO:0000768
rhabdomyosarcoma1MONDO:0005212EFO:0002918
anaplastic large cell lymphoma1MONDO:0020325EFO:0003032
head and neck cancer1MONDO:0005627EFO:0006859
Sezary syndrome1MONDO:0017844EFO:1000785
mycosis fungoides1MONDO:0009691EFO:1001051
mantle cell lymphoma1MONDO:0018876EFO:1001469
scleroderma1MONDO:0019340EFO:1001993
Waldenstrom macroglobulinemia1MONDO:0100280EFO:0009441
central nervous system neoplasm1MONDO:0006130EFO:1000158
peritoneal neoplasm1MONDO:0006901MONDO:0002087
fallopian tube neoplasm1MONDO:0021092MONDO:0002158
myeloid leukemia1MONDO:0004643MONDO:0004643
ovarian cancer1MONDO:0008170MONDO:0008170
follicular lymphoma1MONDO:0018906MONDO:0018906
nasal cavity and paranasal sinus lethal midline granuloma1MONDO:0006828MONDO:0019472
Alzheimer disease1MONDO:0004975MONDO:0004975
peripheral T-cell lymphoma, not otherwise specified1MONDO:0004964EFO:0000211
colorectal neoplasm1MONDO:0005335MONDO:0005575
endometrium neoplasm0MONDO:0021251MONDO:0011962

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

Clinical trials

Total trials: 316.

Phase distribution

PhaseTrials
PHASE2157
PHASE170
PHASE1/PHASE234
Not specified21
PHASE314
PHASE410
PHASE2/PHASE36
EARLY_PHASE14

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03844360PHASE4RECRUITINGDose Individualization of Antineoplastic Drugs and Anti-Infective Drug in Children With Hematoplastic Disease
NCT04877522PHASE4RECRUITINGAsciminib Roll-over Study
NCT05944783PHASE4NOT_YET_RECRUITINGBioequivalence Studies of Dasatinib 100 Mg
NCT07046182PHASE4ACTIVE_NOT_RECRUITINGClinical Study of CEP+Dasatinib + Azacytidine in First-line Treatment of. Angioimmunoblastoma Foresight
NCT01660906PHASE4COMPLETEDPhase IV, Open-label, Multicenter Study of Dasatinib in Chronic-Phase Chronic Myeloid Leukemia (CP-CML) Patients With Chronic, Low-grade Non-Hematologic Toxicity to Imatinib
NCT02690922PHASE4UNKNOWNLow-dose Chemotherapy Combine With Tyrosine Kinase Inhibitor to Treat ph+ Acute Lymphoblastic Leukemia Patients
NCT03216070PHASE4UNKNOWNLow-dose Dasatinib as First-line Treatment for Chronic Myeloid Leukemia
NCT04155411PHASE4UNKNOWNDose Reduced Dasatinib (70 mg Daily) as First-line Treatment for Newly Diagnosed CML-CP
NCT04925141PHASE4COMPLETEDA Study of Dasatinib as First-line Treatment for Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia (CML-CP)
NCT04933526PHASE4UNKNOWNThe Efficacy and Safety of Switching to Flumatinib Versus Dasatinib After Imatinib-related Low-grade Adverse Events in CML-CP Patients
NCT03020030PHASE3ACTIVE_NOT_RECRUITINGTreatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Children and Adolescents
NCT03117751PHASE2/PHASE3ACTIVE_NOT_RECRUITINGTotal Therapy XVII for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia and Lymphoma
NCT04530565PHASE3ACTIVE_NOT_RECRUITINGTesting the Use of Steroids and Tyrosine Kinase Inhibitors With Blinatumomab or Chemotherapy for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia in Adults
NCT04971226PHASE3ACTIVE_NOT_RECRUITINGA Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
NCT05653258PHASE2/PHASE3RECRUITINGSingle Nuclei RNA-seq to Map Adipose Cellular Populations and Senescent Cells in Older Subjects
NCT06855810PHASE2/PHASE3RECRUITINGNewly-diagnosed Pediatric T-cell ALL Protocol
NCT00123474PHASE3COMPLETEDChronic Myelogenous Leukemia (CML) - Follow on: Study of BMS-354825 in Subjects With CML
NCT00123487PHASE3COMPLETEDAdvanced Chronic Myelogenous Leukemia (CML) - Follow On: Study of BMS-354825 in Subjects With CML
NCT00349518PHASE2/PHASE3WITHDRAWNStudy of Dasatinib in Imatinib Resistant or Intolerant Subjects With Chronic or Advanced Phase CML or Philadelphia Chromosome Positive ALL
NCT00362466PHASE3TERMINATEDA Study of Dasatinib vs. High-Dose Imatinib (600 mg) in Patients With Chronic Phase Chronic Myeloid Leukemia (CML) Who Failed to Achieve Complete Cytogenetic Response After 3-18 Months of Imatinib Therapy
NCT00481247PHASE3COMPLETEDA Phase III Study of Dasatinib vs Imatinib in Patients With Newly Diagnosed Chronic Phase Chronic Myeloid Leukemia
NCT00549848PHASE3COMPLETEDTotal Therapy Study XVI for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia
NCT00720109PHASE2/PHASE3COMPLETEDDasatinib and Combination Chemotherapy in Treating Young Patients With Newly Diagnosed Acute Lymphoblastic Leukemia
NCT00744497PHASE3COMPLETEDRandomized Study Comparing Docetaxel Plus Dasatinib to Docetaxel Plus Placebo in Castration-resistant Prostate Cancer
NCT01460693PHASE3COMPLETEDComparison of Imatinib Versus Dasatinib in Patients With Newly-diagnosed Chronic Phase Chronic Myeloid Leukaemia
NCT02013648PHASE3COMPLETEDRandomized Phase III Study of Intensive Chemotherapy With or Without Dasatinib (Sprycel™)
NCT02326311PHASE3COMPLETEDOptimization of TKIs Treatment and Quality of Life in Ph+ CML Patients ≥60 Years in Deep Molecular Response
NCT02883049PHASE3COMPLETEDCombination Chemotherapy in Treating Young Patients With Newly Diagnosed High-Risk B Acute Lymphoblastic Leukemia and Ph-Like TKI Sensitive Mutations
NCT02890784PHASE3COMPLETEDDasatinib Holiday for Improved Tolerability
NCT03564470PHASE2/PHASE3UNKNOWNPrecision Diagnosis Directing HDACi and TKI Target Therapy for Adult Ph-like ALL
NCT00070499PHASE2ACTIVE_NOT_RECRUITINGImatinib Mesylate or Dasatinib in Treating Patients With Previously Untreated Chronic Phase Chronic Myelogenous Leukemia
NCT00792948PHASE2ACTIVE_NOT_RECRUITINGCombination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia
NCT01990196PHASE2ACTIVE_NOT_RECRUITINGNeoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer
NCT02143414PHASE2ACTIVE_NOT_RECRUITINGBlinatumomab and Combination Chemotherapy or Dasatinib, Prednisone, and Blinatumomab in Treating Older Patients With Acute Lymphoblastic Leukemia
NCT02465060PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02559778PHASE2RECRUITINGPediatric Precision Laboratory Advanced Neuroblastoma Therapy
NCT02689440PHASE2ACTIVE_NOT_RECRUITINGDasatinib and Venetoclax in Treating Patients With Philadelphia Chromosome Positive or BCR-ABL1 Positive Early Chronic Phase Chronic Myelogenous Leukemia
NCT03297606PHASE2RECRUITINGCanadian Profiling and Targeted Agent Utilization Trial (CAPTUR)
NCT03516279PHASE2ACTIVE_NOT_RECRUITINGPembrolizumab and Dasatinib, Imatinib Mesylate, or Nilotinib in Treating Patients With Chronic Myeloid Leukemia and Persistently Detectable Minimal Residual Disease
NCT03654768PHASE2ACTIVE_NOT_RECRUITINGTesting the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia

Clinical evidence (CIViC)

Variant × indication × effect (223 predictive associations from 297 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
BCR::ABL1 FusionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponseDasatinibCIViC AEID11235
BCR::ABL1 FusionChronic Myeloid LeukemiaSensitivity/ResponseNilotinib + DasatinibCIViC AEID261
BCR::ABL1 Fusion AND ABL1 MutationAcute Lymphoblastic LeukemiaSensitivity/ResponseDasatinibCIViC AEID11341
BCR::ABL1 Fusion AND ABL1 TKD MutationChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC AEID11342
ABL1 I418SChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC BEID4715
ARID1A Loss OR ARID1A WildtypeOvarian Clear Cell CarcinomaSensitivity/ResponseDasatinibCIViC BEID11789
ETV6::ABL1 FusionMyeloid NeoplasmSensitivity/ResponseImatinib + Dasatinib + NilotinibCIViC BEID11326
KIT MutationCore Binding Factor Acute Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC BEID8576
BCR::ABL1 Fusion AND ABL1 F317LChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID6309 +6
BCR::ABL1 Fusion AND ABL1 T315IChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4365 +5
BCR::ABL1 Fusion AND ABL1 Y253HChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4335 +3
BCR::ABL1 Fusion AND ABL1 E255VChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4447 +2
BCR::ABL1 Fusion AND ABL1 E355GChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4403 +2
BCR::ABL1 Fusion AND ABL1 F359VChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID3819 +2
BCR::ABL1 Fusion AND ABL1 M244VChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4302 +2
BCR::ABL1 Fusion AND ABL1 M351TChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4396 +2
BCR::ABL1 Fusion AND ABL1 E255KChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4350 +1
BCR::ABL1 Fusion AND ABL1 E459KChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID6310 +1
BCR::ABL1 Fusion AND ABL1 F359IChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4532 +1
BCR::ABL1 Fusion AND ABL1 F486SChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4571 +1
BCR::ABL1 Fusion AND ABL1 G250EChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4316 +1
BCR::ABL1 Fusion AND ABL1 H396RChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID4413 +1
BCR::ABL1 Fusion AND ABL1 L248VChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID6308 +1
ABL1 TKD MutationChronic Myeloid LeukemiaResistanceDasatinibCIViC BEID6311
BCR::ABL1 Fusion AND ABL1 H396RChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC CEID4414 +3
BCR::ABL1 Fusion AND ABL1 Y253FChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC CEID4343 +3
BCR::ABL1 Fusion AND ABL1 E255KChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC CEID4351 +2
BCR::ABL1 Fusion AND ABL1 H396PChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC CEID4556 +2
BCR::ABL1 Fusion AND ABL1 Y253HChronic Myeloid LeukemiaSensitivity/ResponseDasatinibCIViC CEID4333 +2
RCSD1::ABL1 FusionB-lymphoblastic Leukemia/lymphomaSensitivity/ResponseDasatinibCIViC CEID9164 +2

+193 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 5 clinical and 8 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.

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

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
BOSUTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
ERLOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
FEDRATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
GEFITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
IMATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
LAPATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
MIDOSTAURINChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
NERATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
NILOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
PONATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
SORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
SUNITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
VANDETANIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3, SRC
LESTAURTINIBChEMBLPhase 3ABL1, SIK1, SIK2, SIK3, SRC
IdelalisibPubChemApprovedABL1, SIK1, SIK2, SIK3, SRC
SelumetinibPubChemApprovedABL1, SIK1, SIK2, SIK3, SRC
AXITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3
CABOZANTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
CERITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
dacomitinibChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
ENTRECTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
IBRUTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
QUIZARTINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3
REGORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
RUXOLITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK2, SIK3
TIRBANIBULINChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3, SRC
TIVOZANIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK3, SRC
NINTEDANIBChEMBLPhase 4 (approved)ABL1, SIK1, SIK2, SRC
CANERTINIBChEMBLPhase 3ABL1, SIK2, SIK3, SRC
SARACATINIBChEMBLPhase 3ABL1, SIK2, SIK3, SRC
AT-9283ChEMBLPhase 2ABL1, SIK2, SIK3, SRC
FORETINIBChEMBLPhase 2ABL1, SIK1, SIK2, SRC
MILCICLIBChEMBLPhase 2ABL1, SIK2, SIK3, SRC
OSI-632ChEMBLPhase 2ABL1, SIK2, SIK3, SRC
R-406ChEMBLPhase 2ABL1, SIK1, SIK2, SRC
SU-014813ChEMBLPhase 2ABL1, SIK1, SIK2, SRC
TOZASERTIBChEMBLPhase 2ABL1, SIK1, SIK2, SRC
BinimetinibPubChemApprovedABL1, SIK2, SIK3, SRC
FostamatinibPubChemApprovedABL1, SIK2, SIK3, SRC
BRIGATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SRC
DABRAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3
LENVATINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3
TOFACITINIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK1, SIK3
TOVORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, SIK2, SIK3
CEDIRANIBChEMBLPhase 3ABL1, SIK2, SRC
DOVITINIBChEMBLPhase 3ABL1, SIK2, SRC
BMS-690514ChEMBLPhase 2ABL1, SIK2, SRC
DANUSERTIBChEMBLPhase 2ABL1, SIK2, SRC
PELITINIBChEMBLPhase 2ABL1, SIK2, SRC
AcalabrutinibPubChemApprovedSIK1, SIK2, SIK3
DuvelisibPubChemApprovedSIK1, SIK2, SIK3
SirolimusPubChemApprovedSIK1, SIK2, SIK3
TrametinibPubChemApprovedABL1, SIK2, SIK3
MOMELOTINIBChEMBL + PubChemPhase 4 (approved)SIK2, SIK3
RIBOCICLIBChEMBL + PubChemPhase 4 (approved)SIK2, SIK3
INFIGRATINIBChEMBLPhase 4 (approved)ABL1, SRC
ALISERTIBChEMBLPhase 3ABL1, SRC

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot