Orelabrutinib

Summary

Orelabrutinib (CHEMBL4650321) is a phase-3 clinical-stage small molecule (ATC L01EL04) targeting BTK; indicated across 15 conditions including b-cell chronic lymphocytic leukemia and mantle cell lymphoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: L01EL04
• Targets: 1 (BTK)
• Indications: 15 conditions
• Clinical trials: 83
• Chemistry: 427.5 Da · C26H25N3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4650321
Name	Orelabrutinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	91667513
ATC	L01EL04
Molecular formula	C26H25N3O3
Molecular weight	427.5
InChIKey	MZPVEMOYADUARK-UHFFFAOYSA-N

SMILES: C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4

IUPAC name: 2-(4-phenoxyphenyl)-6-(1-prop-2-enoylpiperidin-4-yl)pyridine-3-carboxamide

Also known as: Icp-022, ICP-022, ICP022, Innobruka, Orelabrutinib, ORELABRUTINIB

Patent coverage: 155 distinct patent families (364 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 296 (81%) 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
BTK	Bruton tyrosine kinase	Inhibition	8.36	0.7%	Q06187

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Epidermal growth factor receptor, Tyrosine-protein kinase Tec, Tyrosine-protein kinase BTK.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 6 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
BTK	8.8	IC50	1.6	nM	CHEMBL_ACT_25033556
BTK	8.36	IC50	4.4	nM	CHEMBL_ACT_28707299
BTK	8.36	IC50	4.4	nM	CHEMBL_ACT_28707449
BTK	7.7	IC50	20	nM	CHEMBL_ACT_25067002
TEC	7.43	IC50	37.2	nM	CHEMBL_ACT_25067059
EGFR	5.23	IC50	5900	nM	CHEMBL_ACT_25067049

Target pathways

Aggregated over 1 target gene(s): BTK.

Top Reactome pathways

45 total, by targets touching each:

Pathway	Targets	Genes
ER-Phagosome pathway	1	BTK
Antigen processing-Cross presentation	1	BTK
Adaptive Immune System	1	BTK
Signal Transduction	1	BTK
Disease	1	BTK
Toll Like Receptor 4 (TLR4) Cascade	1	BTK
MyD88:MAL(TIRAP) cascade initiated on plasma membrane	1	BTK
Toll Like Receptor TLR1:TLR2 Cascade	1	BTK
Toll Like Receptor TLR6:TLR2 Cascade	1	BTK
Innate Immune System	1	BTK
Immune System	1	BTK
Toll-like Receptor Cascades	1	BTK
Toll Like Receptor 2 (TLR2) Cascade	1	BTK
Signaling by Rho GTPases	1	BTK
RHO GTPase Effectors	1	BTK
Fcgamma receptor (FCGR) dependent phagocytosis	1	BTK
Regulation of actin dynamics for phagocytic cup formation	1	BTK
DAP12 interactions	1	BTK
DAP12 signaling	1	BTK
Fc epsilon receptor (FCERI) signaling	1	BTK
FCERI mediated Ca+2 mobilization	1	BTK
Signaling by GPCR	1	BTK
GPCR downstream signalling	1	BTK
G-protein beta:gamma signalling	1	BTK
G alpha (q) signalling events	1	BTK
G alpha (12/13) signalling events	1	BTK
Diseases of Immune System	1	BTK
Diseases associated with the TLR signaling cascade	1	BTK
MyD88 deficiency (TLR2/4)	1	BTK
IRAK4 deficiency (TLR2/4)	1	BTK
Infectious disease	1	BTK
RHO GTPases Activate WASPs and WAVEs	1	BTK
G beta:gamma signalling through BTK	1	BTK
Leishmania infection	1	BTK
Parasite infection	1	BTK
Leishmania phagocytosis	1	BTK
FCGR3A-mediated phagocytosis	1	BTK
Potential therapeutics for SARS	1	BTK
SARS-CoV Infections	1	BTK
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1	BTK
Parasitic Infection Pathways	1	BTK
Viral Infection Pathways	1	BTK
Class I MHC mediated antigen processing & presentation	1	BTK
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers	1	BTK
Signaling by the B Cell Receptor (BCR)	1	BTK

Dominant GO biological processes

GO term	Targets
neutrophil homeostasis	1
positive regulation of type III hypersensitivity	1
positive regulation of type I hypersensitivity	1
adaptive immune response	1
B cell affinity maturation	1
histamine secretion by mast cell	1
positive regulation of immunoglobulin production	1
regulation of B cell cytokine production	1
MyD88-dependent toll-like receptor signaling pathway	1
regulation of B cell apoptotic process	1
mesoderm development	1
peptidyl-tyrosine phosphorylation	1
calcium-mediated signaling	1
proteoglycan catabolic process	1
negative regulation of B cell proliferation	1

Indications & clinical

Indications

14 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
B-cell chronic lymphocytic leukemia	3	MONDO:0004948	EFO:0000095
mantle cell lymphoma	3	MONDO:0018876	EFO:1001469
diffuse large B-cell lymphoma	3	MONDO:0018905	EFO:0000403
neoplasm	3	MONDO:0005070	EFO:0000616
marginal zone lymphoma	3	MONDO:0017604	EFO:1000630
relapsing-remitting multiple sclerosis	2	MONDO:0005314	EFO:0003929
neoplasm of mature B-cells	2	MONDO:0004949	EFO:0000096
autoimmune thrombocytopenic purpura	2	MONDO:0008558	EFO:0007160
Waldenstrom macroglobulinemia	2	MONDO:0100280	EFO:0009441
follicular lymphoma	2	MONDO:0018906	MONDO:0018906
systemic lupus erythematosus	2	MONDO:0007915	MONDO:0007915
lymphoma	2	MONDO:0005062	EFO:0000574
Hodgkins lymphoma	1	MONDO:0004952	EFO:0000183
liver disorder	1	MONDO:0005154	EFO:0001421

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

Clinical trials

Total trials: 83.

Phase distribution

Phase	Trials
PHASE2	47
PHASE3	13
PHASE1/PHASE2	7
Not specified	7
PHASE1	6
PHASE2/PHASE3	2
PHASE4	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07355699	PHASE4	RECRUITING	Application of Orelabrutinib With or Without CD20 Monoclonal Antibody in Previously Untreated Marginal Zone Lymphoma
NCT05351346	PHASE3	RECRUITING	Genotype-guided Treatment in DLBCL
NCT06004856	PHASE3	RECRUITING	Evaluate the Efficacy and Safety of Orelabrutinib in Adult Patients With Chronic Primary Immune Thrombocytopenia
NCT06082102	PHASE3	RECRUITING	Efficacy and Safety of Orelabrutinib Combined With Rituximab Versus Lenalidomide Combined With Rituximab in Patients With Relapsed/Refractory Marginal Zone Lymphoma
NCT06363994	PHASE3	RECRUITING	A Global Phase 3 Study of Orelabrutinib+BR Vs.BR in Pts with TN MCL
NCT06378138	PHASE2/PHASE3	RECRUITING	ICP-248 in Combination With Orelabrutinib in Treatment-naïve Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (APEX-03)
NCT06496308	PHASE3	RECRUITING	Bendamustine and Rituximab With or Without Orelabrutinib in MCL Treatment
NCT07067463	PHASE3	RECRUITING	A Study of Orelabrutinib in Patients With Primary Progressive Multiple Sclerosis
NCT07185373	PHASE2/PHASE3	NOT_YET_RECRUITING	Orelabrutinib Combined With Teniposide, Rituximab and Methotrexate for Newly Diagnosed PCNSL
NCT07299019	PHASE3	RECRUITING	A Study of Orelabrutinib in Patients With Secondary Progressive Multiple Sclerosis
NCT07377578	PHASE3	RECRUITING	A Study of Rocbrutinib Versus Investigator’s Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma
NCT04578613	PHASE3	UNKNOWN	ICP-022 Versus Chlorambucil Combined With Rituximab in the Treatment of Untreated CLL/SLL
NCT05051891	PHASE3	COMPLETED	A Randomized, Open-label, Multi-center, Phase III Study of Orelabrutinib in Combination With Rituximab, Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone (R-CHOP) vs. R-CHOP Alone in Patients With Treatment-naїve Mantle Cell Lymphoma
NCT05097443	PHASE3	UNKNOWN	Orelabrutinib, Rituximab and Combination Chemotherapy in Newly-diagnosed Aggressive B-cell Non-Hodgkin Lymphoma
NCT05234684	PHASE3	UNKNOWN	A Study of Orelabrutinib Plus R-CHOP in Treatment-naïve Patients With MCD Subtype Diffuse Large B-cell Lymphoma
NCT05334238	PHASE3	UNKNOWN	Orelabrutinib Maintenance Therapy After ASCT in Primary Central Nervous System Lymphoma
NCT04961515	PHASE2	RECRUITING	Orelabrutinib, Sintilimab and Temozolomide in Relapsed or Refractory Central Nervous System Lymphoma
NCT04989621	PHASE2	RECRUITING	Orelabrutinib Plus Rituximab Followed by Maintenance With Orelabrutinib for Relapsed and Refractory Follicular Lymphoma(RR FL)
NCT05209620	PHASE2	RECRUITING	Orelabrutinib Combined With Pemetrexed For Relapsed/Refractory Central Nervous System Lymphoma
NCT05600660	PHASE2	RECRUITING	Orelabrutinib,Rituximab and Methotrexate in Newly Diagnosed Primary Central Nervous System Lymphoma
NCT05688696	PHASE2	RECRUITING	Evaluate the Efficacy and Safety of Orelabrutinib in Adult Patients With Systemic Lupus Erythematosus
NCT05933967	PHASE2	RECRUITING	A Study of Orelabrutinib Plus R-CHOP in Treatment-naïve Patients With Double Expression Diffuse Large B-cell Lymphoma
NCT06228963	PHASE2	RECRUITING	Orelabrutinib in the Treatment of HP-positive Gastric MALT Lymphoma
NCT06454968	PHASE2	RECRUITING	Orelabrutinib Combined With Obinutuzumab and Lenalidomide (OGL Regimen) as First-line Treatment for Marginal Zone Lymphoma.
NCT06476899	PHASE2	NOT_YET_RECRUITING	A Practical Clinical Study Comparing the Fixed-cycle Regimen Containing Orelabrutinib With BTKi Monotherapy
NCT06503276	PHASE2	RECRUITING	The Treatment of Ocular Adnexal Extranodal Marginal Zone B-cell Lymphoma by Orelabrutinib and Radiotherapy
NCT06513234	PHASE2	RECRUITING	Combination of Orelabrutinib and Obinutuzumab in Untreated Marginal Zone Lymphomas
NCT06516978	PHASE2	NOT_YET_RECRUITING	A Study Comparing the Efficacy and Safety of Pola-RCHP-X Versus RCHOP-X and Pola-RCHP in Previously Untreated Patients With DLBCL
NCT06530511	PHASE2	RECRUITING	Polatuzumab, Rituximab and Orelabrutinib Combination Regimen (PRO) in the Treatment of Elderly Frail Patients with Treatment-naive Non-GCB DLBCL
NCT06566807	PHASE2	RECRUITING	Oxygen Study-Orelabrutinib Combined With Obinutuzumab(O2) for First-Line Treatment of Marginal Zone Lymphoma
NCT06583837	PHASE2	ACTIVE_NOT_RECRUITING	Orelabrutinib Followed by Response-adapted Ultra-low Dose 4Gy Radiation as First-line Treatment of MALT Lymphoma
NCT06647940	PHASE2	RECRUITING	Orelabrutinib in Combination with R-CHOP for CD5-positive DLBCL Patients（Rocket Trial）
NCT06656221	PHASE2	NOT_YET_RECRUITING	A Prospective, Single-Center Study Evaluating the Efficacy and Safety of Glofitamab Combined With Orelabrutinib and Bortezomib in Patients With High-Risk Mantle Cell Lymphoma
NCT06700798	PHASE2	RECRUITING	Orelabrutinib Combined With Rituximab Versus R-CVP in the Untreated MZL： A Randomized, Open Phase II Trial
NCT06701357	PHASE2	RECRUITING	CR-CHOP+X in Previously Untreated DEL
NCT06793189	PHASE2	RECRUITING	MZL-IPI Risk-adapted Targeted Therapy in Untreated MZL
NCT06901999	PHASE2	NOT_YET_RECRUITING	Methotrexate or Thiotepa Combined With R-CHOP and Orelabrutinib in CNSL Patients
NCT07199296	PHASE2	RECRUITING	Orelabrutinib and Rituximab With Optional Autologous Hematopoietic Stem Cell Transplantation in MCL Treatment
NCT07208981	PHASE2	RECRUITING	Orelabrutinib Combined With Zebetuzumab and Lenalidomide for the Treatment of Newly Diagnosed MZL
NCT07247383	PHASE2	ACTIVE_NOT_RECRUITING	Orelabrutinib Plus Low-Dose Radiotherapy Or Rituximab For Ocular Adnexal MALT Lymphoma
NCT07272499	PHASE2	RECRUITING	Orelabrutinib Plus Lisaftoclax and Rituximab in Untreated Mantle Cell Lymphoma With High-Risk Disease
NCT07400250	PHASE2	NOT_YET_RECRUITING	Phase II Study of Orelabrutinib in Combination With Romiplostim N01 in Patients With Primary Immune Thrombocytopenia (ITP) Who Have Received At Least One Prior Line of Therapy
NCT07410520	PHASE2	RECRUITING	PD-1 Inhibitor Combined With Rituximab, Methotrexate, and Orelabrutinib (PD-1i+RMO) for Newly Diagnosed PCNSL and SCNSL.
NCT07441993	PHASE2	RECRUITING	Exploratory Study of Orelabrutinib in the Treatment of Early-stage Untreated MZL
NCT07448324	PHASE2	RECRUITING	Orelabrutinib Combined With Rituximab ± Lenalidomide in Response-Adapted Stratified Therapy for Untreated MZL
NCT07480863	PHASE2	ACTIVE_NOT_RECRUITING	Treatment of Orelabrutinib+Hi-CVP Regimen for Previously Untreated MZL
NCT07499271	PHASE2	RECRUITING	Genetic Subtype-matched Targeted Therapy for the Treatment of Newly Diagnosed DLBCL With TP53 Mutation
NCT07554898	PHASE2	RECRUITING	Ultra-low-dose Radiation Therapy Followed by Orelabrutinib as First-line Treatment for Stage Ⅰ-Ⅱ MALT Lymphoma
NCT07585747	PHASE2	NOT_YET_RECRUITING	A Exploratory Study on Untreated Follicular Lymphoma With Orelabrutinib, Tafasitamab, and Lenalidomide
NCT03493217	PHASE1/PHASE2	UNKNOWN	A Study to Evaluate ICP-022 in Patients With CLL/ SLL
NCT03494179	PHASE1/PHASE2	UNKNOWN	A Study to Evaluate ICP-022 in Patients With R/R Mantle Cell Lymphoma (MCL)
NCT03797456	PHASE2	COMPLETED	A Study to Evaluate ICP-022 in Patients With R/R Marginal Zone Lymphoma (MZL)
NCT04014205	PHASE1/PHASE2	UNKNOWN	A Study of Tyrosine Kinase Inhibitor Orelabrutinib (ICP-022) in Patients With r/r B-Cell Malignancies
NCT04304040	PHASE1/PHASE2	UNKNOWN	A Study of MIL62 Combined With Orelabrutinib for the Treatment of R/R CD20+B Cell Lymphoma
NCT04305197	PHASE1/PHASE2	COMPLETED	A Study of ICP-022 in Patients With Systemic Lupus Erythematosus (SLE)
NCT04438005	PHASE2	COMPLETED	A Study of ICP-022 in Patients With R/R DLBCL
NCT04438044	PHASE2	UNKNOWN	A Study to Evaluate ICP-022 in Patients With R/R PCNSL and SCNSL
NCT04440059	PHASE2	COMPLETED	A Study of ICP-022 in the Treatment of Recurrent or Refractory Waldenstrom Macroglobulinemia
NCT04711148	PHASE2	UNKNOWN	A Phase 2 Study of Orelabrutinib in Patients With Relapsing-Remitting Multiple Sclerosis
NCT04899427	PHASE2	UNKNOWN	Phase II Study of Orelabrutinib Combined With PD-1 Inhibitor in Relapsed/Refractory Primary Central Nervous System Lymphoma
NCT05014100	PHASE2	UNKNOWN	Orelabrutinib in Combination With R2 Regimen for R/R CD20+ B-cell Lymphoma
NCT05020288	PHASE2	UNKNOWN	A Clinical Trial of the Orelabrutinib in the Management of Refractory ITP
NCT05021770	PHASE1/PHASE2	UNKNOWN	Orelabrutinib in Combination With Thiotepa in Refractory and Relapsed Primary CNS Lymphoma
NCT05124028	PHASE1/PHASE2	UNKNOWN	A Study of Orelabrutinib in Patients With ITP
NCT05322733	PHASE2	UNKNOWN	Orelabrutinib and Obinutuzumab Plus FC Regimen in Treating Newly Diagnosed CLL/SLL
NCT05381506	PHASE2	UNKNOWN	Study of Orelabrutinib in Combination With Gemox in Refractory / Relapsed Diffuse Large B-cell Lymphoma
NCT05390749	PHASE2	UNKNOWN	Sequential Treatment With RO-MTX After Pomalidomide, Orelabrutinib, Rituximab (POR) in Newly-diagnosed PCNSL
NCT05491044	PHASE2	UNKNOWN	A Study of Orelabrutinib in CLL/SLL Patients Who Are Slowly Responding to Ibrutinib
NCT05498259	PHASE2	UNKNOWN	Orelabrutinib With R-CHOP-like Regimen for Patients With Newly Diagnosed Untreated Non-GCB DLBCL
NCT05926427	PHASE2	UNKNOWN	Orelabrutinib Combined With Rituximab and Chemotherapy for Relapsed/Refractory B-Cell Lymphoma Patients With Central Nervous System Involvement
NCT05036577	PHASE1	ACTIVE_NOT_RECRUITING	A Dose-escalating Pilot Study of Orelabrutinib for Newly-diagnosed PCNSL
NCT05728658	PHASE1	RECRUITING	The Study of ICP-248 in Patients With Mature B-cell Malignancies
NCT03189017	PHASE1	COMPLETED	A Phase I Study of ICP-022 in Healthy Subjects
NCT05316857	PHASE1	COMPLETED	DDI Study of Orelabrutinib
NCT05660720	PHASE1	UNKNOWN	Evaluate the Effect of Orelabrutinib on Cardiac Repolarization in Healthy Subjects
NCT05684653	PHASE1	UNKNOWN	Study to Evaluate Orelabrutinib Tablets in Subjects With Hepatic Impairment and Healthy Subject
NCT05809180	Not specified	RECRUITING	Pro-miniCHOP-like Regimen for Treatment-naive Elderly Patients
NCT07257510	Not specified	RECRUITING	Pomalidomide Plus Orelabrutinib and Zuberitamab in Untreated Mantle Cell Lymphoma
NCT05284175	Not specified	UNKNOWN	A Study of Orelabrutinib in Patients With AQP4-IgG Positive Neuromyelitis Optica Spectrum Disorder
NCT05495828	Not specified	UNKNOWN	Orelabrutinib Therapy in Patients With r/r B-cell Lymphoma Intolerant to Other Bruton Tyrosine Kinase Inhibitors
NCT05920668	Not specified	UNKNOWN	Phase IV Observational Study of Orelabrutinib in the Treatment of Chronic Lymphocytic Leukemia/Small Cell Lymphoma
NCT06015464	Not specified	UNKNOWN	An Ambispective Cohort Study of Orelabrutinib in Combination With Standard Treatment Regimen for Untreated DLBCL
NCT06115824	Not specified	COMPLETED	New-diagnosed PCNSL Treated With Methotrexate (MTX) and Orelabrutinib-based Regimen

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

80 molecules share ≥1 primary target. Top 80 by shared-target count:

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	BTK
BOSUTINIB	ChEMBL	Phase 4 (approved)	BTK
BRIGATINIB	ChEMBL	Phase 4 (approved)	BTK
CERITINIB	ChEMBL	Phase 4 (approved)	BTK
DASATINIB	ChEMBL	Phase 4 (approved)	BTK
ENTRECTINIB	ChEMBL	Phase 4 (approved)	BTK
FEDRATINIB	ChEMBL	Phase 4 (approved)	BTK
FUTIBATINIB	ChEMBL	Phase 4 (approved)	BTK
IBRUTINIB	ChEMBL	Phase 4 (approved)	BTK
MITOXANTRONE	ChEMBL	Phase 4 (approved)	BTK
NERATINIB	ChEMBL	Phase 4 (approved)	BTK
NINTEDANIB	ChEMBL	Phase 4 (approved)	BTK
OLMUTINIB	ChEMBL	Phase 4 (approved)	BTK
OSIMERTINIB	ChEMBL	Phase 4 (approved)	BTK
PIRTOBRUTINIB	ChEMBL	Phase 4 (approved)	BTK
PONATINIB	ChEMBL	Phase 4 (approved)	BTK
SUNITINIB	ChEMBL	Phase 4 (approved)	BTK
TIRABRUTINIB	ChEMBL	Phase 4 (approved)	BTK
VANDETANIB	ChEMBL	Phase 4 (approved)	BTK
ZANUBRUTINIB	ChEMBL	Phase 4 (approved)	BTK
ABIVERTINIB	ChEMBL	Phase 3	BTK
ALISERTIB	ChEMBL	Phase 3	BTK
CANERTINIB	ChEMBL	Phase 3	BTK
CEDIRANIB	ChEMBL	Phase 3	BTK
DOVITINIB	ChEMBL	Phase 3	BTK
ENTOSPLETINIB	ChEMBL	Phase 3	BTK
EVOBRUTINIB	ChEMBL	Phase 3	BTK
FENEBRUTINIB	ChEMBL	Phase 3	BTK
LESTAURTINIB	ChEMBL	Phase 3	BTK
NEMTABRUTINIB	ChEMBL	Phase 3	BTK
POZIOTINIB	ChEMBL	Phase 3	BTK
PYROTINIB	ChEMBL	Phase 3	BTK
REMIBRUTINIB	ChEMBL	Phase 3	BTK
RILZABRUTINIB	ChEMBL	Phase 3	BTK
ROCILETINIB	ChEMBL	Phase 3	BTK
SARACATINIB	ChEMBL	Phase 3	BTK
TESEVATINIB	ChEMBL	Phase 3	BTK
TOLEBRUTINIB	ChEMBL	Phase 3	BTK
APITOLISIB	ChEMBL	Phase 2	BTK
AT-9283	ChEMBL	Phase 2	BTK
ATUZABRUTINIB	ChEMBL	Phase 2	BTK
BIIB-091	ChEMBL	Phase 2	BTK
BMS-754807	ChEMBL	Phase 2	BTK
BMS-919373	ChEMBL	Phase 2	BTK
BMS-986142	ChEMBL	Phase 2	BTK
BRANEBRUTINIB	ChEMBL	Phase 2	BTK
CENISERTIB	ChEMBL	Phase 2	BTK
CEP-11981	ChEMBL	Phase 2	BTK
DANUSERTIB	ChEMBL	Phase 2	BTK
DEFOSBARASERTIB	ChEMBL	Phase 2	BTK
EDRALBRUTINIB	ChEMBL	Phase 2	BTK
ELSUBRUTINIB	ChEMBL	Phase 2	BTK
FORETINIB	ChEMBL	Phase 2	BTK
ILORASERTIB	ChEMBL	Phase 2	BTK
MILREBRUTINIB	ChEMBL	Phase 2	BTK
PELITINIB	ChEMBL	Phase 2	BTK
POSELTINIB	ChEMBL	Phase 2	BTK
R-406	ChEMBL	Phase 2	BTK
REBASTINIB	ChEMBL	Phase 2	BTK
SOFNOBRUTINIB	ChEMBL	Phase 2	BTK
SOQUELITINIB	ChEMBL	Phase 2	BTK
SPEBRUTINIB	ChEMBL	Phase 2	BTK
SU-014813	ChEMBL	Phase 2	BTK
TOZASERTIB	ChEMBL	Phase 2	BTK
UCN-01	ChEMBL	Phase 2	BTK
VECABRUTINIB	ChEMBL	Phase 2	BTK
ZELEBRUDOMIDE	ChEMBL	Phase 2	BTK
Afatinib	PubChem	Approved	BTK
belumosudil	PubChem	Approved	BTK
Binimetinib	PubChem	Approved	BTK
dacomitinib	PubChem	Approved	BTK
Fostamatinib	PubChem	Approved	BTK
Idelalisib	PubChem	Approved	BTK
Mobocertinib	PubChem	Approved	BTK
Pazopanib	PubChem	Approved	BTK
regorafenib	PubChem	Approved	BTK
Selumetinib	PubChem	Approved	BTK
Trametinib	PubChem	Approved	BTK