Bosutinib

Summary

Bosutinib (CHEMBL288441) is an approved small-molecule antineoplastic agent (ATC L01EA04) targeting CAMK2G, ABL1, and CAMK1D; indicated across 20 conditions including neoplasm and chronic myeloid leukemia; with CIViC clinical evidence for 73 variant-indication associations (e.g. BCR::ABL1 Fusion in chronic myeloid leukemia).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EA04
• Targets: 16 (CAMK2G, ABL1, CAMK1D…)
• Indications: 20 conditions
• Clinical trials: 60
• Precision-oncology evidence (CIViC): 73 variant–indication associations
• Chemistry: 530.4 Da · C26H29Cl2N5O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL288441
Name	Bosutinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5328940
ChEBI	CHEBI:39112
ATC	L01EA04
Molecular formula	C26H29Cl2N5O3
Molecular weight	530.4
InChIKey	UBPYILGKFZZVDX-UHFFFAOYSA-N

SMILES: CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

IUPAC name: 4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile

ChEBI definition: An aminoquinoline that is 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline bearing additional cyano and methoxy substituents at positions 3 and 6 respectively.

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

Also known as: Bosutinib, SK-606, SKI-606, bosutinib, BOSUTINIB, SID124950167, BosutinibÊ, BosutinibÂ

Parent form; salt/anhydrous children: CHEMBL2095206, CHEMBL2131134

Patent coverage: 4,956 distinct patent families (12,255 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 11,276 (92%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CAMK2G	calcium/calmodulin-dependent protein kinase II gamma subunit	Inhibition	6.74	0.3%	Q13555
ABL1	ABL proto-oncogene 1, non-receptor tyrosine kinase	Inhibition	9	1.2%	P00519
CAMK1D	calcium/calmodulin dependent protein kinase ID	Inhibition	7.04	0.1%	Q8IU85
FRK	fyn related Src family tyrosine kinase	Inhibition	8.66	0%	P42685
FYN	FYN proto-oncogene, Src family tyrosine kinase	Inhibition	8.74	0%	P06241
LYN	LYN proto-oncogene, Src family tyrosine kinase	Inhibition	8.1	0.5%	P07948
MAP4K5	mitogen-activated protein kinase kinase kinase kinase 5	Inhibition	9.52	0%	Q9Y4K4
SIK1	salt inducible kinase 1	Inhibition	8.52	1%	P57059
SIK2	salt inducible kinase 2	Inhibition	8.52	0.5%	Q9H0K1
SIK3	SIK family kinase 3	Inhibition	7.74	1.3%	Q9Y2K2
SRC	SRC proto-oncogene, non-receptor tyrosine kinase	Inhibition	9	3.7%	P12931
STK10	serine/threonine kinase 10		7.28	0%	O94804
STK24	serine/threonine kinase 24	Inhibition	8.41	0.1%	Q9Y6E0
STK4	serine/threonine kinase 4	Inhibition	6.72	0.2%	Q13043
TNK2	tyrosine kinase non receptor 2	Inhibition	8.57	0%	Q07912
TXK	TXK tyrosine kinase	Inhibition	9.52	0.7%	P42681

Broader ChEMBL bioactivity targets: 237 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase TAO2, STE20/SPS1-related proline-alanine-rich protein kinase, Mitogen-activated protein kinase kinase kinase 13, Microtubule-associated serine/threonine-protein kinase 1, Serine/threonine-protein kinase VRK2, Vasopressin V2 receptor, Hormonally up-regulated neu tumor-associated kinase.

Bioactivity

ChEMBL activities: 468 potent at pChembl ≥ 5 of 480 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ABL1	10.54	Kd	0.03	nM	CHEMBL_ACT_7593139
ABL1	10.44	Kd	0.04	nM	CHEMBL_ACT_7593147
ABL1	10.43	Kd	0.04	nM	CHEMBL_ACT_7593142
ABL1	10.41	Kd	0.04	nM	CHEMBL_ACT_7593144
ABL1	10.33	Kd	0.05	nM	CHEMBL_ACT_7593135
ABL1	10.24	Kd	0.06	nM	CHEMBL_ACT_7593141
ABL1	10.24	Kd	0.06	nM	CHEMBL_ACT_7593149
ABL1	10.21	Kd	0.06	nM	CHEMBL_ACT_7593140
ABL1	10.1	IC50	0.08	nM	CHEMBL_ACT_29170874
ABL1	10.07	Kd	0.09	nM	CHEMBL_ACT_7593143
ABL1	10	Kd	0.1	nM	CHEMBL_ACT_16565695
ABL1	9.96	Kd	0.11	nM	CHEMBL_ACT_7593138
ABL1	9.92	Kd	0.12	nM	CHEMBL_ACT_7593148
ABL1	9.74	Kd	0.18	nM	CHEMBL_ACT_7593137
MAP4K5	9.52	IC50	0.3	nM	CHEMBL_ACT_3446183
YES1	9.4	IC50	0.4	nM	CHEMBL_ACT_3446182
ABL1	9.3	IC50	0.5	nM	CHEMBL_ACT_3446181
ABL2	9.3	IC50	0.5	nM	CHEMBL_ACT_3446186
MAP4K5	9.3	Kd	0.5	nM	CHEMBL_ACT_7594756
LCK	9.23	Kd	0.59	nM	CHEMBL_ACT_7594707
ABL1	9.2	Kd	0.63	nM	CHEMBL_ACT_7593136
ERBB3	9.11	Kd	0.77	nM	CHEMBL_ACT_29275975
ERBB3	9.11	Kd	0.77	nM	CHEMBL_ACT_7593005
ABL1	9	IC50	1	nM	CHEMBL_ACT_1600031
SRC	9	Kd	1	nM	CHEMBL_ACT_16510625
SRC	9	Kd	1	nM	CHEMBL_ACT_16565685
BMX	9	IC50	1	nM	CHEMBL_ACT_16595580
MAP2K1	9	IC50	1	nM	CHEMBL_ACT_16595581
ABL1	9	IC50	1	nM	CHEMBL_ACT_16595582
SRC	9	IC50	1	nM	CHEMBL_ACT_16595583

Target pathways

Aggregated over 16 target gene(s): CAMK2G, ABL1, CAMK1D, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK.

Top Reactome pathways

241 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	7	ABL1, CAMK2G, LYN, SRC, STK10, STK4, TNK2
Immune System	5	ABL1, CAMK2G, LYN, SRC, STK10
Disease	4	ABL1, CAMK2G, LYN, SRC
FCGR3A-mediated phagocytosis	4	ABL1, FYN, LYN, SRC
Hemostasis	3	ABL1, LYN, SRC
Developmental Biology	3	ABL1, LYN, SRC
Cytokine Signaling in Immune system	3	CAMK2G, LYN, SRC
Signaling by SCF-KIT	3	FYN, LYN, SRC
Regulation of KIT signaling	3	FYN, LYN, SRC
Innate Immune System	3	ABL1, LYN, STK10
Signaling by Rho GTPases	3	ABL1, SRC, STK10
FCGR activation	3	FYN, LYN, SRC
PECAM1 interactions	3	FYN, LYN, SRC
Generic Transcription Pathway	3	ABL1, CAMK2G, SRC
EPH-Ephrin signaling	3	FYN, LYN, SRC
Co-stimulation by CD28	3	FYN, LYN, SRC
Co-inhibition by CTLA4	3	FYN, LYN, SRC
EPHB-mediated forward signaling	3	FYN, LYN, SRC
EPHA-mediated growth cone collapse	3	FYN, LYN, SRC
EPH-ephrin mediated repulsion of cells	3	FYN, LYN, SRC
Axon guidance	3	ABL1, LYN, SRC
Diseases of signal transduction by growth factor receptors and second messengers	3	CAMK2G, LYN, SRC
Infectious disease	3	ABL1, LYN, SRC
RAF/MAP kinase cascade	3	CAMK2G, FYN, SRC
Cyclin D associated events in G1	3	ABL1, LYN, SRC
RNA Polymerase II Transcription	3	ABL1, CAMK2G, SRC
Gene expression (Transcription)	3	ABL1, CAMK2G, SRC
Signaling by Receptor Tyrosine Kinases	3	LYN, SRC, TNK2
FCGR3A-mediated IL10 synthesis	3	FYN, LYN, SRC
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	3	FYN, LYN, SRC

Dominant GO biological processes

GO term	Targets
protein phosphorylation	16
intracellular signal transduction	11
protein autophosphorylation	8
signal transduction	6
cell differentiation	5
Fc-gamma receptor signaling pathway involved in phagocytosis	4
ephrin receptor signaling pathway	4
immune system process	4
regulation of gene expression	3
response to xenobiotic stimulus	3
positive regulation of apoptotic process	3
T cell receptor signaling pathway	3
cellular response to hydrogen peroxide	3
cellular response to transforming growth factor beta stimulus	3
apoptotic process	3

Indications & clinical

Indications

20 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).

Indication	Trial phase	MONDO	EFO
neoplasm	3	MONDO:0005070	EFO:0000616
chronic myeloid leukemia	3	MONDO:0011996	EFO:0000339
glioblastoma	2	MONDO:0018177	EFO:0000519
leukemia	2	MONDO:0005059	EFO:0000565
breast carcinoma	2	MONDO:0004989	EFO:0000305
autosomal dominant polycystic kidney disease	2	MONDO:0004691	EFO:1001496
breast neoplasm	2	MONDO:0021100	MONDO:0007254
exocrine pancreatic carcinoma	1	MONDO:0005192	EFO:0002618
dementia	1	MONDO:0001627	HP:0000726
mesothelioma	1	MONDO:0005065	EFO:0000588
non-small cell lung carcinoma	1	MONDO:0005233	EFO:0003060
thymoma	1	MONDO:0006456	EFO:1000581
blast phase chronic myelogenous leukemia, BCR-ABL1 positive	1	MONDO:0006115	EFO:1000131
peritoneal neoplasm	1	MONDO:0006901	MONDO:0002087
ovarian cancer	1	MONDO:0008170	MONDO:0008170
amyotrophic lateral sclerosis	1	MONDO:0004976	MONDO:0004976

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

Clinical trials

Total trials: 60.

Phase distribution

Phase	Trials
PHASE1	27
PHASE2	17
Not specified	6
PHASE3	5
PHASE1/PHASE2	3
PHASE4	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04877522	PHASE4	RECRUITING	Asciminib Roll-over Study
NCT02228382	PHASE4	TERMINATED	Safety And Efficacy Study Of Bosutinib In Patients With Philadelphia Chromosome Positive Chronic Myeloid Leukemia Previously Treated With One Or More Tyrosine Kinase Inhibitors
NCT04971226	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
NCT06423911	PHASE3	RECRUITING	Study of Olverembatinib (HQP1351) in Patients With CP-CML
NCT00574873	PHASE3	COMPLETED	Compare Bosutinib To Imatinib In Subjects With Newly Diagnosed Chronic Phase Philadelphia Chromosome Positive CML
NCT02130557	PHASE3	COMPLETED	A Multicenter Phase 3, Open-Label Study of Bosutinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia
NCT03106779	PHASE3	COMPLETED	Study of Efficacy of CML-CP Patients Treated With ABL001 Versus Bosutinib, Previously Treated With 2 or More TKIs
NCT03297606	PHASE2	RECRUITING	Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR)
NCT03654768	PHASE2	ACTIVE_NOT_RECRUITING	Testing the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia
NCT04258943	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Bosutinib in Pediatric Patients With Newly Diagnosed Chronic Phase or Resistant/Intolerant Ph + Chronic Myeloid Leukemia
NCT00261846	PHASE2	COMPLETED	Study Evaluating SKI-606 (Bosutinib) In Philadelphia Chromosome Positive Leukemias
NCT00319254	PHASE2	COMPLETED	Study Evaluating SKI-606 (Bosutinib) In Subjects With Breast Cancer
NCT00793546	PHASE2	TERMINATED	Study Evaluating Bosutinib-Exemestane Combination Vs Exemestane Alone in Post Menopausal Women With Breast Cancer
NCT00811070	PHASE2	COMPLETED	Study Evaluating SKI-606 (Bosutinib) In Japanese Subjects With Philadelphia Chromosome Positive Leukemias
NCT00880009	PHASE2	TERMINATED	Study Evaluating Bosutinib-Letrozole Combination Versus Letrozole Alone In Post Menopausal Women With Breast Cancer
NCT00959946	PHASE1/PHASE2	TERMINATED	Study Of Bosutinib With Capecitabine In Solid Tumors And Locally Advanced Or Metastatic Breast Cancer
NCT01233869	PHASE2	COMPLETED	Bosutinib For Autosomal Dominant Polycystic Kidney Disease
NCT01331291	PHASE2	COMPLETED	Bosutinib in Adult Patients With Recurrent Glioblastoma
NCT02311998	PHASE1/PHASE2	COMPLETED	Phase I/II Study of Bosutinib in Combination With Inotuzumab Ozogamicin in CD22-positive PC Positive ALL and CML
NCT02445742	PHASE2	COMPLETED	CML Treated With Bosutinib After Relapse
NCT02638467	PHASE2	COMPLETED	Allogeneic Stem Cell Transplantation in Chronic Myeloid Leukemia Failing TKIs Therapy
NCT02810990	PHASE2	COMPLETED	Bosutinib in Elderly Chronic Myeloid Leukemia
NCT02906696	PHASE2	TERMINATED	Bosutinib in Treating Patients With Chronic Myeloid Leukemia in Chronic Phase After Frontline TKI Failure
NCT03128411	PHASE2	COMPLETED	Study of Bosutinib in Japanese Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia
NCT03831776	PHASE2	COMPLETED	Long-acting Low Dose Ropeginterferon for Chronic Myeloid Leukemia Treated With Bosutinib From Diagnosis
NCT03888222	PHASE2	COMPLETED	Impact of Bosutinib on Safety, Tolerability, Biomarkers and Clinical Outcomes in Dementia With Lewy Bodies
NCT04578847	PHASE2	UNKNOWN	A Study of REduction And DIscontinuation Treatment of TKI (Imatinib, Nilotinib, Dasatinib and Bosutinib)
NCT00195260	PHASE1	COMPLETED	Study Evaluating SKI-606 (Bosutinib) In Advanced Malignant Solid Tumors
NCT00406406	PHASE1	COMPLETED	Study Evaluating SKI-606 Administered to Healthy Subjects
NCT00434486	PHASE1	COMPLETED	Study Evaluating Drug Interaction Between Multiple Doses of Ketoconazole and a Single Dose of SKI-606
NCT00499538	PHASE1	COMPLETED	Study Evaluating 3 New Formulations of SKI-606 in Healthy Adult Subjects
NCT00721474	PHASE1	COMPLETED	Study to Determine the Effect of a High-Fat Meal on the Relative Bioavailability and Pharmacokinetics of a Single Dose of Bosutinib Administered Orally to Healthy Subjects
NCT00725426	PHASE1	COMPLETED	Effect of Rifampin on Bosutinib When Both Are Given to Healthy People
NCT00757341	PHASE1	COMPLETED	Study Evaluating The Mass Balance And Metabolic Disposition Of SKI-606
NCT00759837	PHASE1	COMPLETED	Study Evaluating The Pharmacokinetics (PK) And Safety Of Bosutinib In Subjects With Liver Disease And In Healthy Subjects
NCT00777530	PHASE1	COMPLETED	Study Evaluating Ascending Single-Dose Of Bosutinib Administered With Multiple Doses Of Ketoconazole To Healthy Subjects
NCT00914121	PHASE1	COMPLETED	Study Evaluating The Effect of Bosutinib (SKI-606) On Cardiac Repolarization (Rhythms Of The Heart)
NCT00934674	PHASE1	COMPLETED	Study Comparing Two Different Tablet Formulations Of Bosutinib
NCT00952913	PHASE1	COMPLETED	Study Evaluating The Potential Effect Of Lansoprazole On The Pharmacokinetics Of Bosutinib In Healthy Subjects
NCT01001936	PHASE1	COMPLETED	Study Evaluating SKI-606 in Subject With Solid Tumors

Clinical evidence (CIViC)

Variant × indication × effect (73 predictive associations from 91 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
BCR::ABL1 Fusion	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC A	EID11224
BCR::ABL1 Fusion	B-lymphoblastic Leukemia/lymphoma	Sensitivity/Response	Bosutinib	CIViC A	EID11287
BCR::ABL1 Fusion AND ABL1 TKD Mutation	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC A	EID11289
BCR::ABL1 Fusion AND ABL1 M351T	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC B	EID4393 +1
ABL1 TKD Mutation OR ABL1 P-Loop Mutation OR ABL1 Non-P-Loop Mutation	Acute Lymphoblastic Leukemia	Sensitivity/Response	Bosutinib	CIViC B	EID11339
ABL1 Non-P-Loop Mutation	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC B	EID6337 +1
ABL1 P-Loop Mutation	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC B	EID6336 +1
ABL1 TKD Mutation	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC B	EID6335 +1
BCR::ABL1 Fusion AND ABL1 D421G	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC C	EID4559
BCR::ABL1 Fusion AND ABL1 L387F	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC C	EID4553
BCR::ABL1 Fusion AND ABL1 N331S	Chronic Myeloid Leukemia	Sensitivity/Response	Bosutinib	CIViC C	EID4550
BCR::ABL1 Fusion AND ABL1 E255V	Chronic Myeloid Leukemia	Reduced Sensitivity	Bosutinib	CIViC C	EID4444
BCR::ABL1 Fusion AND ABL1 F317L	Chronic Myeloid Leukemia	Reduced Sensitivity	Bosutinib	CIViC C	EID4382
BCR::ABL1 Fusion AND ABL1 G250E	Chronic Myeloid Leukemia	Reduced Sensitivity	Bosutinib	CIViC C	EID4314
BCR::ABL1 Fusion AND ABL1 M351T	Chronic Myeloid Leukemia	Reduced Sensitivity	Bosutinib	CIViC C	EID4394
BCR::ABL1 Fusion AND ABL1 V299L	Chronic Myeloid Leukemia	Reduced Sensitivity	Bosutinib	CIViC C	EID4538
BCR::ABL1 Fusion AND ABL1 E255K	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4347 +2
BCR::ABL1 Fusion AND ABL1 T315I	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4362 +2
ABL1 F486Y	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4569 +1
BCR::ABL1 Fusion AND ABL1 F317L	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4381 +1
BCR::ABL1 Fusion AND ABL1 F359I	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4530 +1
BCR::ABL1 Fusion AND ABL1 F359V	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID3815 +1
BCR::ABL1 Fusion AND ABL1 G250E	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4313 +1
BCR::ABL1 Fusion AND ABL1 H396R	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4410 +1
BCR::ABL1 Fusion AND ABL1 L248V	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4310 +1
BCR::ABL1 Fusion AND ABL1 M244V	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4307 +1
BCR::ABL1 Fusion AND ABL1 Y253F	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4340 +1
BCR::ABL1 Fusion AND ABL1 Y253H	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4331 +1
ABL1 C475V	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4768
ABL1 L298V	Chronic Myeloid Leukemia	Resistance	Bosutinib	CIViC C	EID4475

+43 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

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

Related molecules

Related molecules

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.

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

Molecule	Source	Status	Shared targets
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Erlotinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Sorafenib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
LESTAURTINIB	ChEMBL	Phase 3	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Idelalisib	PubChem	Approved	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Selumetinib	PubChem	Approved	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Dasatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK4, TNK2, TXK
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK4, TNK2, TXK
Vandetanib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TXK
Entrectinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2
Ibrutinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TXK
Lapatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2, TXK
Quizartinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, LYN, MAP4K5, SIK1, SIK2, SIK3, STK10, STK24, STK4, TNK2, TXK
NINTEDANIB	ChEMBL	Phase 4 (approved)	ABL1, CAMK1D, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SRC, STK10, STK24, STK4, TNK2, TXK
SU-014813	ChEMBL	Phase 2	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SRC, STK10, STK24, STK4, TNK2
TOZASERTIB	ChEMBL	Phase 2	ABL1, CAMK1D, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SRC, STK10, STK24, STK4, TNK2, TXK
Ponatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SIK3, SRC, STK10, STK4, TNK2
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2
RUXOLITINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK1D, CAMK2G, FRK, MAP4K5, SIK1, SIK2, SIK3, STK10, STK24, STK4, TNK2, TXK
FORETINIB	ChEMBL	Phase 2	ABL1, CAMK1D, FRK, FYN, LYN, MAP4K5, SIK1, SIK2, SRC, STK10, STK4, TNK2, TXK
PELITINIB	ChEMBL	Phase 2	ABL1, CAMK1D, FRK, FYN, LYN, MAP4K5, SIK2, SRC, STK10, STK24, STK4, TNK2, TXK
Binimetinib	PubChem	Approved	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2
Fostamatinib	PubChem	Approved	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2
dacomitinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK4, TNK2
Tirbanibulin	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4, TNK2
R-406	ChEMBL	Phase 2	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, SIK1, SIK2, SRC, STK10, TNK2, TXK
Trametinib	PubChem	Approved	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, STK10, STK24, STK4, TNK2
Cabozantinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, STK24, STK4
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, FRK, FYN, LYN, SIK1, SIK2, SIK3, SRC, STK10, STK24, TXK
DOVITINIB	ChEMBL	Phase 3	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SRC, STK10, STK24, STK4
Cobimetinib	PubChem	Approved	CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, STK10, STK24, STK4, TNK2
AXITINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, MAP4K5, SIK1, SIK2, SIK3, STK10, STK24, STK4, TNK2, TXK
BRIGATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, FYN, LYN, SIK2, SRC, STK10, STK24, TXK
CANERTINIB	ChEMBL	Phase 3	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, TXK
SARACATINIB	ChEMBL	Phase 3	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10, TNK2
BMS-690514	ChEMBL	Phase 2	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SIK2, SRC, STK10, TNK2
DANUSERTIB	ChEMBL	Phase 2	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SRC, STK10, STK4, TNK2
DABRAFENIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, FRK, FYN, LYN, SIK2, SIK3, STK10, STK24, STK4
MOMELOTINIB	ChEMBL + PubChem	Phase 4 (approved)	CAMK1D, CAMK2G, FRK, MAP4K5, SIK2, SIK3, STK10, STK24, STK4
Tovorafenib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, CAMK2G, FRK, MAP4K5, SIK2, SIK3, STK10, STK24, STK4
CEDIRANIB	ChEMBL	Phase 3	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SRC, STK10, STK4
MILCICLIB	ChEMBL	Phase 2	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, TNK2
OSI-632	ChEMBL	Phase 2	ABL1, FRK, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10
ABEMACICLIB	ChEMBL + PubChem	Phase 4 (approved)	CAMK1D, CAMK2G, SIK2, SIK3, STK10, STK24, STK4, TXK
TIVOZANIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, FRK, LYN, SIK1, SIK3, SRC, STK10, TXK
LINIFANIB	ChEMBL	Phase 3	ABL1, CAMK2G, FRK, LYN, MAP4K5, SRC, STK10, STK4
AT-9283	ChEMBL	Phase 2	ABL1, FYN, LYN, MAP4K5, SIK2, SIK3, SRC, STK10
CENISERTIB	ChEMBL	Phase 2	ABL1, CAMK2G, FRK, FYN, LYN, MAP4K5, SRC, TNK2
ILORASERTIB	ChEMBL	Phase 2	ABL1, CAMK1D, CAMK2G, FRK, FYN, LYN, SRC, TNK2
REBASTINIB	ChEMBL	Phase 2	ABL1, FRK, FYN, LYN, MAP4K5, SRC, STK10, STK4
Capivasertib	PubChem	Approved	CAMK2G, FRK, MAP4K5, SIK2, SIK3, STK10, STK24, STK4
Pexidartinib	PubChem	Approved	CAMK2G, FRK, MAP4K5, SIK2, SIK3, STK10, STK24, STK4
BARICITINIB	ChEMBL + PubChem	Phase 4 (approved)	CAMK2G, FRK, SIK2, SIK3, STK10, STK24, STK4