Acalabrutinib

Summary

Acalabrutinib (CHEMBL3707348) is an approved small-molecule EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor (ATC L01EL02) targeting EGFR, ERBB4, and BLK; indicated across 24 conditions including b-cell chronic lymphocytic leukemia and mantle cell lymphoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EL02
• Targets: 14 (EGFR, ERBB4, BLK…)
• Indications: 24 conditions
• Clinical trials: 143
• Chemistry: 465.5 Da · C26H23N7O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3707348
Name	Acalabrutinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	71226662
ChEBI	CHEBI:167707
ATC	L01EL02
Molecular formula	C26H23N7O2
Molecular weight	465.5
InChIKey	WDENQIQQYWYTPO-IBGZPJMESA-N

SMILES: CC#CC(=O)N1CCC[C@H]1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5

IUPAC name: 4-[8-amino-3-[(2S)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide

ChEBI definition: A member of the class of imidazopyrazines that is imidazo[1,5-a]pyrazine substituted by 4-(pyridin-2-ylcarbamoyl)phenyl, (2S)-1-(but-2-ynoyl)pyrrolidin-2-yl, and amino groups at positions 1, 3 and 8, respectively. It is an irreversible second-generation Bruton’s tyrosine kinase (BTK) inhibitor that is approved by the FDA for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.

Pharmacological roles (ChEBI): EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, antineoplastic agent, apoptosis inducer.

Also known as: Acalabrutinib, Acp-196, ACP-196, ACALABRUTINIB, acalabrutinib, Acalabrutinib; Calquence

Parent form; salt/anhydrous children: CHEMBL4594293

Patent coverage: 1,845 distinct patent families (4,504 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 4,454 (99%) 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
EGFR	epidermal growth factor receptor	Inhibition	6	17.5%	P00533
ERBB4	erb-b2 receptor tyrosine kinase 4	Inhibition	7.8	0.7%	Q15303
BLK	BLK proto-oncogene, Src family tyrosine kinase	Inhibition	6	0.1%	P51451
BMX	BMX non-receptor tyrosine kinase	Inhibition	7.34	0%	P51813
BTK	Bruton tyrosine kinase	Inhibition	8	0.7%	Q06187
ERBB2	erb-b2 receptor tyrosine kinase 2	Inhibition	6	17.7%	P04626
FYN	FYN proto-oncogene, Src family tyrosine kinase	Inhibition	6	0%	P06241
ITK	IL2 inducible T cell kinase	Inhibition	6	0%	Q08881
JAK3	Janus kinase 3	Inhibition	6	0.6%	P52333
LCK	LCK proto-oncogene, Src family tyrosine kinase	Inhibition	6	0.1%	P06239
LYN	LYN proto-oncogene, Src family tyrosine kinase	Inhibition	6	0.5%	P07948
SRC	SRC proto-oncogene, non-receptor tyrosine kinase	Inhibition	6	3.7%	P12931
TEC	tec protein tyrosine kinase	Inhibition	7.03	0.1%	P42680
TXK	TXK tyrosine kinase	Inhibition	6.43	0.7%	P42681

Broader ChEMBL bioactivity targets: 14 (assay-derived). Sample: Receptor tyrosine-protein kinase erbB-2, Epidermal growth factor receptor, Tyrosine-protein kinase JAK3, Tyrosine-protein kinase Blk, Prostaglandin G/H synthase 2, Adenosine receptor A3, Vascular endothelial growth factor receptor 2, Tyrosine-protein kinase ITK/TSK, Receptor tyrosine-protein kinase erbB-4, Platelet glycoprotein VI.

Bioactivity

ChEMBL activities: 66 potent at pChembl ≥ 5 of 68 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
BTK	8.59	Kd	2.6	nM	CHEMBL_ACT_24797370
BTK	8.52	IC50	3	nM	CHEMBL_ACT_18415137
BTK	8.52	IC50	3	nM	CHEMBL_ACT_19052356
BTK	8.52	IC50	3	nM	CHEMBL_ACT_24703137
BTK	8.52	IC50	3	nM	CHEMBL_ACT_25030289
BTK	8.52	IC50	3	nM	CHEMBL_ACT_25033554
BTK	8.52	IC50	3	nM	CHEMBL_ACT_26133916
BTK	8.51	IC50	3.1	nM	CHEMBL_ACT_16606455
BTK	8.51	IC50	3.1	nM	CHEMBL_ACT_22877421
BTK	8.29	IC50	5.1	nM	CHEMBL_ACT_24805898
BTK	8.29	IC50	5.1	nM	CHEMBL_ACT_24954226
BTK	8.29	IC50	5.1	nM	CHEMBL_ACT_26283443
BTK	8.29	IC50	5.1	nM	CHEMBL_ACT_26315204
TEC	8.26	Kd	5.5	nM	CHEMBL_ACT_24797394
ERBB2	8.13	Kd	7.4	nM	CHEMBL_ACT_19061212
BTK	8.04	EC50	9.2	nM	CHEMBL_ACT_24805910
BTK	7.96	IC50	11	nM	CHEMBL_ACT_25067001
TEC	7.85	Kd	14	nM	CHEMBL_ACT_19061194
ERBB4	7.8	IC50	16	nM	CHEMBL_ACT_22877451
ERBB4	7.8	IC50	16	nM	CHEMBL_ACT_24956646
ERBB4	7.8	IC50	16	nM	CHEMBL_ACT_26315218
BLK	7.75	Kd	18	nM	CHEMBL_ACT_24797358
BTK	7.73	IC50	18.6	nM	CHEMBL_ACT_28780871
BTK	7.72	IC50	19	nM	CHEMBL_ACT_19061025
BMX	7.72	Kd	19	nM	CHEMBL_ACT_24797364
TEC	7.7	IC50	20	nM	CHEMBL_ACT_25067058
BTK	7.68	Kd	21	nM	CHEMBL_ACT_19061182
BTK	7.63	IC50	23.5	nM	CHEMBL_ACT_23299050
BTK	7.62	IC50	24	nM	CHEMBL_ACT_19061055
TXK	7.62	Kd	24	nM	CHEMBL_ACT_24797400

Target pathways

Aggregated over 14 target gene(s): EGFR, ERBB4, BLK, BMX, BTK, ERBB2, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK.

Top Reactome pathways

277 total, by targets touching each:

Pathway	Targets	Genes
Immune System	8	BLK, BTK, ITK, JAK3, LCK, LYN, SRC, TEC
PIP3 activates AKT signaling	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
Signal Transduction	6	BTK, JAK3, LCK, LYN, SRC, TEC
Constitutive Signaling by Aberrant PI3K in Cancer	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
RAF/MAP kinase cascade	6	EGFR, ERBB2, ERBB4, FYN, JAK3, SRC
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
Signaling by ERBB2	5	EGFR, ERBB2, ERBB4, FYN, SRC
Cytokine Signaling in Immune system	5	JAK3, LCK, LYN, SRC, TEC
Adaptive Immune System	5	BLK, BTK, ITK, LCK, LYN
Signaling by SCF-KIT	5	FYN, LCK, LYN, SRC, TEC
Disease	5	BTK, JAK3, LCK, LYN, SRC
Innate Immune System	5	BTK, ITK, LCK, LYN, TEC
FCERI mediated Ca+2 mobilization	5	BTK, ITK, LYN, TEC, TXK
Infectious disease	5	BTK, JAK3, LCK, LYN, SRC
Signaling by Receptor Tyrosine Kinases	5	JAK3, LCK, LYN, SRC, TEC
Regulation of KIT signaling	4	FYN, LCK, LYN, SRC
PECAM1 interactions	4	FYN, LCK, LYN, SRC
Fc epsilon receptor (FCERI) signaling	4	BTK, ITK, LYN, TEC
Co-stimulation by CD28	4	FYN, LCK, LYN, SRC
Co-inhibition by CTLA4	4	FYN, LCK, LYN, SRC
Signaling by Interleukins	4	JAK3, LCK, LYN, TEC
FCGR3A-mediated phagocytosis	4	BTK, FYN, LYN, SRC
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	4	FYN, LCK, LYN, SRC
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers	4	BLK, BTK, FYN, LYN
Hemostasis	3	LCK, LYN, SRC
GPVI-mediated activation cascade	3	FYN, LCK, LYN
Signaling by ERBB4	3	EGFR, ERBB4, SRC
SHC1 events in ERBB2 signaling	3	EGFR, ERBB2, ERBB4
Signaling by Rho GTPases	3	BTK, LCK, SRC
GRB2 events in ERBB2 signaling	3	EGFR, ERBB2, ERBB4

Dominant GO biological processes

GO term	Targets
protein phosphorylation	14
intracellular signal transduction	11
peptidyl-tyrosine phosphorylation	8
adaptive immune response	8
immune system process	8
signal transduction	7
cell surface receptor protein tyrosine kinase signaling pathway	7
B cell receptor signaling pathway	7
T cell receptor signaling pathway	6
cell surface receptor signaling pathway	5
positive regulation of MAPK cascade	5
protein autophosphorylation	5
epidermal growth factor receptor signaling pathway	4
negative regulation of apoptotic process	4
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	4

Indications & clinical

Indications

24 indications (4 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
B-cell chronic lymphocytic leukemia	4	MONDO:0004948	EFO:0000095
mantle cell lymphoma	4	MONDO:0018876	EFO:1001469
neoplasm	4	MONDO:0005070	EFO:0000616
diffuse large B-cell lymphoma	3	MONDO:0018905	EFO:0000403
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
non-Hodgkin lymphoma	2	MONDO:0018908	EFO:0005952
Waldenstrom macroglobulinemia	2	MONDO:0100280	EFO:0009441
ovarian cancer	2	MONDO:0008170	MONDO:0008170
follicular lymphoma	2	MONDO:0018906	MONDO:0018906
hematopoietic and lymphoid system neoplasm	2	MONDO:0002334	MONDO:0044881
food allergy	2	MONDO:0700226	EFO:1001890
marginal zone lymphoma	2	MONDO:0017604	EFO:1000630
glioblastoma	1	MONDO:0018177	EFO:0000519
plasma cell myeloma	1	MONDO:0009693	EFO:0001378
prolymphocytic leukemia	1	MONDO:0001023	MONDO:0001023
lymphoma	1	MONDO:0005062	EFO:0000574
infectious disease	1	MONDO:0005550	EFO:0005741
leukemia	1	MONDO:0005059	EFO:0000565

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

Clinical trials

Total trials: 143.

Phase distribution

Phase	Trials
PHASE2	73
PHASE1	22
PHASE1/PHASE2	20
PHASE3	19
Not specified	5
PHASE4	2
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06651970	PHASE4	RECRUITING	Acalabrutinib Monotherapy vs Investigator’s Choice of Treatment in Patients With CL Leukaemia and Heart Failure
NCT04930536	PHASE4	COMPLETED	Acalabrutinib Study in Indian Patients With Chronic Lymphocytic Leukaemia & Relapsed and Refractory Mantle Cell Lymphoma
NCT02475681	PHASE3	ACTIVE_NOT_RECRUITING	Acalabrutinib, Obinutuzumab and Chlorambucil in Treatment naïve CLL
NCT02477696	PHASE3	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib (ACP-196) Versus Ibrutinib in Previously Treated Participants With High Risk Chronic Lymphocytic Leukemia (CLL)
NCT02970318	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Acalabrutinib vs Investigator’s Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL
NCT02972840	PHASE3	ACTIVE_NOT_RECRUITING	A Study of BR Alone Versus in Combination With Acalabrutinib in Subjects With Previously Untreated MCL
NCT03836261	PHASE3	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib (ACP-196) in Combination With Venetoclax (ABT-199), With and Without Obinutuzumab (GA101) Versus Chemoimmunotherapy for Previously Untreated CLL
NCT03868722	PHASE2/PHASE3	RECRUITING	Acalabrutinib and Venetoclax Treatment of Newly Diagnosed Patients With CLL at High Risk of Infection or Early Treatment
NCT04075292	PHASE3	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib Versus Chlorambucil Plus Rituximab in Adult Subjects With Previously Untreated Chronic Lymphocytic Leukemia
NCT04529772	PHASE3	ACTIVE_NOT_RECRUITING	A Combination of Acalabrutinib With R-CHOP in Subjects With Previously Untreated Non-GCB DLBCL (ACE-LY-312)
NCT04662255	PHASE3	ACTIVE_NOT_RECRUITING	Study of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)
NCT05057494	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Acalabrutinib Plus Venetoclax Versus Venetoclax Plus Obinutuzumab in Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT05197192	PHASE3	RECRUITING	A Phase-3-trial of Acalabrutinib, Obinutuzumab & Venetoclax Compared to Obinutuzumab and Venetoclax in Previously Untreated Patients With High Risk CLL
NCT05820841	PHASE3	RECRUITING	Acalabrutinib in Combination With R-miniCHOP in Older Adults With Untreated Diffuse Large B-Cell Lymphoma
NCT06136559	PHASE3	RECRUITING	A Study of Nemtabrutinib (MK-1026) Versus Comparator (Investigator’s Choice of Ibrutinib or Acalabrutinib) in First Line (1L) Chronic Lymphocytic Leukemia (CLL)/ Small Lymphocytic Lymphoma (SLL) (MK-1026-011/BELLWAVE-011)
NCT06319456	PHASE3	RECRUITING	A Global Study of Lisaftoclax (APG-2575) Combined With Acalabrutinib Versus Immunochemotherapy for Newly Diagnosed CLL/SLL.
NCT06428019	PHASE3	RECRUITING	A Study to Evaluate the Risk of Tumor Lysis Syndrome (TLS) in Adult Participants Receiving Oral Venetoclax in Combination With Intravenously Infused Obinutuzumab or Oral Acalabrutinib for Previously Untreated Chronic Lymphocytic Leukemia (CLL)
NCT07277231	PHASE3	RECRUITING	A Study to Investigate Sonrotoclax (BGB-11417) Plus Zanubrutinib (BGB-3111) Compared With Venetoclax Plus Acalabrutinib in Adults With Previously Untreated Chronic Lymphocytic Leukemia
NCT07377578	PHASE3	RECRUITING	A Study of Rocbrutinib Versus Investigator’s Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma
NCT02735876	PHASE3	WITHDRAWN	A Study of Acalabrutinib in Combination With Rituximab Versus Ibrutinib Versus Acalabrutinib in Subjects With Relapsed or Refractory Mantle Cell Lymphoma
NCT04008706	PHASE3	COMPLETED	Acalabrutinib Safety Study in Untreated and Relapsed or Refractory Chronic Lymphocytic Leukemia Patients
NCT04647669	PHASE3	UNKNOWN	World Health Organization (WHO) COVID-19 Solidarity Trial for COVID-19 Treatments
NCT02029443	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	ACP-196 (Acalabrutinib), a Novel Bruton Tyrosine Kinase (BTK) Inhibitor, for Treatment of Chronic Lymphocytic Leukemia, Richter’s Syndrome or Prolymphocytic Leukemia
NCT02180711	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib Alone or in Combination Therapy in Subjects With B-cell Non-Hodgkin Lymphoma
NCT02180724	PHASE2	ACTIVE_NOT_RECRUITING	An Open-label, Phase 2 Study of ACP-196 in Subjects With Waldenström Macroglobulinemia
NCT02213926	PHASE2	ACTIVE_NOT_RECRUITING	An Open-label, Phase 2 Study of ACP-196 (Acalabrutinib) in Subjects With Mantle Cell Lymphoma
NCT02586857	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Phase 1b/2, Multicenter, Open-label Study of ACP-196 in Subjects With Recurrent Glioblastoma Multiforme (GBM)
NCT02717611	PHASE2	ACTIVE_NOT_RECRUITING	A Study of ACP-196 (Acalabrutinib) in Subjects With Relapsed/Refractory CLL and Intolerant of Ibrutinib Therapy
NCT03128879	PHASE2	RECRUITING	Venetoclax With Ibrutinib or Acalabrutinib in Pts. With High-risk CLL
NCT03516617	PHASE2	RECRUITING	Acalabrutinib With or Without Obinutuzumab in Treating Patients With Early-Stage Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT03571568	PHASE1/PHASE2	RECRUITING	A Study of BI-1206 in Combination With Rituximab With or Without Acalabrutinib in Subjects With Indolent B-Cell NHL
NCT03580928	PHASE2	ACTIVE_NOT_RECRUITING	Acalabrutinib, Venetoclax, and Obinutuzumab for Initial Therapy of CLL
NCT03863184	PHASE2	ACTIVE_NOT_RECRUITING	Acalabrutinib-Lenalidomide-Rituximab in Patients With Untreated MCL
NCT03899337	PHASE2	RECRUITING	A Trial of CHOP-R Therapy, With or Without Acalabrutinib, in Patients With Newly Diagnosed Richter’s Syndrome
NCT03932331	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib in Chinese Adult Subjects With Relapsed or Refractory Mantle Cell Lymphoma, Chronic Lymphocytic Leukemia or Other B-cell Malignancies
NCT03946878	PHASE2	ACTIVE_NOT_RECRUITING	Venetoclax and Acalabrutinib in Treating Patients With Relapsed or Refractory Mantle Cell Lymphoma
NCT04002947	PHASE2	RECRUITING	Acalabrutinib With DA-EPOCH-R or R-CHOP for People With Untreated Diffuse Large B-cell Lymphoma
NCT04115631	PHASE2	ACTIVE_NOT_RECRUITING	A Comparison of Three Chemotherapy Regimens for the Treatment of Patients With Newly Diagnosed Mantle Cell Lymphoma
NCT04169737	PHASE2	RECRUITING	Acalabrutinib and Venetoclax With or Without Early Obinutuzumab for the Treatment of High Risk, Recurrent, or Refractory Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT04189757	PHASE2	ACTIVE_NOT_RECRUITING	Acalabrutinib for the Treatment of Ibrutinib-Intolerant Mantle Cell Lymphoma

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
BOSUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
IBRUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
DASATINIB	ChEMBL	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
CANERTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
R-406	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
ZANUBRUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, TEC, TXK
LESTAURTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
FORETINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, LCK, LYN, SRC, TEC, TXK
PELITINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TXK
Idelalisib	PubChem	Approved	BLK, BMX, BTK, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, FYN, JAK3, LCK, LYN, SRC, TEC, TXK
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, LCK, LYN, SRC, TEC, TXK
TOZASERTIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, FYN, ITK, JAK3, LCK, LYN, SRC, TEC, TXK
BRIGATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, LCK, LYN, SRC, TEC, TXK
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, JAK3, LCK, LYN, SRC, TXK
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, FYN, JAK3, LCK, LYN, SRC, TEC, TXK
CENISERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, ERBB2, ERBB4, FYN, JAK3, LCK, LYN, SRC, TEC
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, FYN, LCK, LYN, SRC, TEC, TXK
MOBOCERTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
REMIBRUTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
ILORASERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, LCK, LYN, SRC
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	BLK, EGFR, ERBB4, FYN, JAK3, LCK, LYN, SRC, TXK
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
NINTEDANIB	ChEMBL	Phase 4 (approved)	BLK, BTK, FYN, ITK, JAK3, LCK, LYN, SRC, TXK
CEDIRANIB	ChEMBL	Phase 3	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, LCK, LYN, SRC
DOVITINIB	ChEMBL	Phase 3	BLK, BTK, EGFR, FYN, ITK, JAK3, LCK, LYN, SRC
ATUZABRUTINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, TEC, TXK
SU-014813	ChEMBL	Phase 2	BLK, BTK, EGFR, FYN, ITK, JAK3, LCK, LYN, SRC
AXITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ITK, JAK3, LCK, TEC, TXK
ENTRECTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, FYN, JAK3, LCK, LYN, SRC, TEC
LAPATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, SRC, TEC, TXK
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, FYN, LCK, LYN, SRC, TEC, TXK
PONATINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, ERBB2, FYN, LCK, LYN, SRC, TEC
TIRABRUTINIB	ChEMBL	Phase 4 (approved)	BLK, BMX, BTK, ERBB2, ERBB4, LCK, TEC, TXK
BMS-986142	ChEMBL	Phase 2	BLK, BMX, BTK, ITK, LCK, SRC, TEC, TXK
BRANEBRUTINIB	ChEMBL	Phase 2	BMX, BTK, EGFR, ERBB4, ITK, JAK3, TEC, TXK
REBASTINIB	ChEMBL	Phase 2	BLK, BMX, BTK, FYN, ITK, LCK, LYN, SRC
SPEBRUTINIB	ChEMBL	Phase 2	BMX, BTK, EGFR, ITK, JAK3, LYN, TEC, TXK
Binimetinib	PubChem	Approved	BTK, EGFR, ERBB2, FYN, LCK, LYN, SRC, TEC
CERITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, JAK3, LCK, LYN, SRC, TEC
QUIZARTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, ITK, LCK, LYN, TEC, TXK
ALISERTIB	ChEMBL	Phase 3	BLK, BTK, EGFR, ERBB2, ERBB4, LCK, SRC
MASITINIB	ChEMBL	Phase 3	BLK, EGFR, ERBB2, FYN, LCK, LYN, SRC
AT-9283	ChEMBL	Phase 2	BTK, FYN, JAK3, LCK, LYN, SRC, TEC
BMS-919373	ChEMBL	Phase 2	BMX, BTK, ITK, JAK3, LCK, LYN, TEC
DEFOSBARASERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, LCK, LYN
OSI-632	ChEMBL	Phase 2	BLK, EGFR, FYN, ITK, LCK, LYN, SRC
belumosudil	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, ERBB2, ERBB4, ITK, JAK3
CABOZANTINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2, LCK, LYN, SRC, TEC
ALVOCIDIB	ChEMBL	Phase 3	EGFR, ERBB2, ERBB4, JAK3, LCK, SRC
EVOBRUTINIB	ChEMBL	Phase 3	BMX, BTK, EGFR, ERBB4, ITK, TEC
SARACATINIB	ChEMBL	Phase 3	BTK, EGFR, FYN, LCK, LYN, SRC