BMX

Summary

BMX (BMX non-receptor tyrosine kinase, HGNC:1079) is a protein-coding gene on chromosome Xp22.2, encoding Cytoplasmic tyrosine-protein kinase BMX (P51813). Non-receptor tyrosine kinase that plays central but diverse modulatory roles in various signaling processes involved in the regulation of actin reorganization, cell migration, cell proliferation and survival, cell adhesion, and apoptosis.

This gene encodes a non-receptor tyrosine kinase belonging to the Tec kinase family. The protein contains a PH-like domain, which mediates membrane targeting by binding to phosphatidylinositol 3,4,5-triphosphate (PIP3), and a SH2 domain that binds to tyrosine-phosphorylated proteins and functions in signal transduction. The protein is implicated in several signal transduction pathways including the Stat pathway, and regulates differentiation and tumorigenicity of several types of cancer cells. Alternatively spliced transcript variants have been found for this gene.

Source: NCBI Gene 660 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 46 total — 1 pathogenic
• Druggable target: yes — 33 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_203281

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1079
Approved symbol	BMX
Name	BMX non-receptor tyrosine kinase
Location	Xp22.2
Locus type	gene with protein product
Status	Approved
Aliases	ETK, PSCTK3
Ensembl gene	ENSG00000102010
Ensembl biotype	protein_coding
OMIM	300101
Entrez	660

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 7 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000342014, ENST00000348343, ENST00000357607, ENST00000463891, ENST00000489983, ENST00000867197, ENST00000867198, ENST00000942875, ENST00000942876

RefSeq mRNA: 3 — MANE Select: NM_203281 NM_001320866, NM_001721, NM_203281

CCDS: CCDS14168

Canonical transcript exons

ENST00000348343 — 19 exons

Exon	Start	End
ENSE00000665865	15546803	15546921
ENSE00000665867	15543071	15543135
ENSE00000665868	15541982	15542198
ENSE00000665871	15534212	15534339
ENSE00000665876	15522346	15522587
ENSE00000665878	15517929	15517993
ENSE00000857421	15508345	15508491
ENSE00001366159	15500807	15500940
ENSE00001434621	15549840	15549997
ENSE00003504267	15516112	15516231
ENSE00003506692	15526042	15526095
ENSE00003526738	15529973	15530027
ENSE00003538151	15511437	15511518
ENSE00003561079	15536353	15536427
ENSE00003604928	15509329	15509433
ENSE00003612261	15531328	15531407
ENSE00003629328	15537134	15537305
ENSE00003651154	15525288	15525365
ENSE00003843797	15556073	15556519

Expression profiles

Bgee: expression breadth ubiquitous, 173 present calls, max score 95.55.

FANTOM5 (CAGE): breadth broad, TPM avg 2.2985 / max 111.5732, expressed in 214 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
195605	1.9813	204
195604	0.1399	60
195606	0.1278	79
195608	0.0312	9
195609	0.0130	1
195607	0.0052	1

Top tissues by expression

289 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
corpus epididymis	UBERON:0004359	95.55	gold quality
right atrium auricular region	UBERON:0006631	79.50	gold quality
cardiac atrium	UBERON:0002081	79.18	gold quality
bone marrow	UBERON:0002371	78.44	gold quality
cardiac muscle of right atrium	UBERON:0003379	78.33	silver quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	76.99	gold quality
right coronary artery	UBERON:0001625	75.77	gold quality
subcutaneous adipose tissue	UBERON:0002190	75.74	gold quality
right lung	UBERON:0002167	74.71	gold quality
calcaneal tendon	UBERON:0003701	74.71	gold quality
urethra	UBERON:0000057	74.66	gold quality
colonic epithelium	UBERON:0000397	74.64	gold quality
mucosa of transverse colon	UBERON:0004991	74.47	gold quality
cauda epididymis	UBERON:0004360	74.45	gold quality
tibial artery	UBERON:0007610	74.39	gold quality
bone marrow cell	CL:0002092	74.35	gold quality
popliteal artery	UBERON:0002250	74.34	gold quality
blood	UBERON:0000178	73.71	gold quality
left ventricle myocardium	UBERON:0006566	73.55	gold quality
aorta	UBERON:0000947	73.17	gold quality
omental fat pad	UBERON:0010414	73.09	gold quality
peritoneum	UBERON:0002358	73.01	gold quality
ascending aorta	UBERON:0001496	72.08	gold quality
thoracic aorta	UBERON:0001515	71.91	gold quality
adipose tissue of abdominal region	UBERON:0007808	71.36	gold quality
left coronary artery	UBERON:0001626	71.34	gold quality
small intestine Peyer’s patch	UBERON:0003454	71.14	gold quality
coronary artery	UBERON:0001621	70.62	gold quality
gall bladder	UBERON:0002110	70.23	gold quality
heart	UBERON:0000948	69.99	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.22
E-MTAB-8410	no	3.07
E-MTAB-6678	no	2.43

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): STAT5A

miRNA regulators (miRDB)

48 targeting BMX, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-338-5P	99.92	72.34	2951
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-3919	99.87	69.45	2489
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-142-5P	99.48	70.92	2416
HSA-MIR-5590-3P	99.48	70.91	2429
HSA-MIR-513A-3P	99.39	70.63	3620
HSA-MIR-513C-3P	99.39	70.63	3620

Literature-anchored findings (GeneRIF, showing 39)

• possible role in regulation of vesicle trafficking (PMID:11877430)
• BMX/Etk is a TNFR2-specific kinase involved in TNF-induced angiogenic events (PMID:12370298)
• Etk activation is essential for transducing the EGF-induced apoptotic signaling in breast cancer cells. (PMID:14676838)
• Pim1 and Etk are required for IL6-induced activation of androgen receptor-mediated transcription in prostate cancer. (PMID:14981536)
• Bmx is a downstream Rap1 effector in VEGF-induced endothelial cell activation. (PMID:15207703)
• two isoforms of Pim-1 kinase may regulate distinct substrates and the 44 kDa Pim-1 may play a more prominent role in drug resistance in prostate cancer cells and interact directly with tyrosine kinase Etk/BMX (PMID:16186805)
• Etk transgenic mouse model may be a useful tool for studying the functions of Etk and identification of new molecular markers and drug targets relevant to human diseases. (PMID:16912182)
• Role of Bmx in ischemia-mediated arteriogenesis/angiogenesis: response to ischemia, enhanced in transgenic mice. (PMID:16932810)
• results demonstrate that Bmx is a critical downstream target of the constitutively active PI 3-kinase in PTEN-deficient PCa cells and further show that Bmx is recruited by the EGF receptor and ErbB3 and activated in response to their respective ligands (PMID:17823122)
• Mechanisms regulating IL-6 production led to the discovery that the Tec kinase bone marrow tyrosine kinase gene in chromosome X (Bmx) regulates Toll-like receptor 4-induced IL-6 production. (PMID:18025155)
• Etk/Bmx may have different biological roles in tumor and nontumor cells, and may be involved in regulating hepatocyte differentiation by c-Fos activation in HCC. (PMID:18196928)
• In fibroblast-like synoviocytes of rheumatoid arthritis patients, Etk is implicated in the cross-talk between focal adhesion kinase (FAK) and myeloid differentiation factor 88 (MyD88) pathways. (PMID:18292575)
• Bmx kinase activity in fibroblasts from rheumatoid synovium is increased following LPS stimulation; Bmx is involved in the regulation of LPS-induced IL-6 and VEGF production via mRNA stabilisation. (PMID:18402776)
• Pretreatment of umbilical vein cells with a pharmacologic inhibitor of Bmx, LFM-A13, produced significant radiosensitization of endothelial cells measured by clonogenic survival analysis and apoptosis. (PMID:18413754)
• BMX is associated with multi-drug resistance of K562/HHT cell line. (PMID:19951526)
• high expression of Etk occurs in 74.6% of SCLC cases, but only in 40% of NSCLC cases, and there is marked difference in the expression levels of Bcl-2, Bcl-X(L) and p53 between Etk-positive and Etk-negative SCLC cases (PMID:20206622)
• by preventing binding of Etk/Bmx to PAR(1) -C-tail, hPar1 oncogenic properties are abrogated (PMID:20559570)
• Investigate Bmx mediates VEGF-dependent lymphangiogenic signaling. (PMID:20864667)
• Etk/BMX may play a role in protection of NPC cells from apoptosis. (PMID:21339702)
• Deregulation of ETK may attribute to the elevated activity of STAT3 and AKT frequently detected in bladder cancer. (PMID:21408190)
• study concludes that BMX is an essential component of inflammatory cytokine signaling and that catalytic, as well as noncatalytic functions of BMX are involved (PMID:21471444)
• Constitutively active STAT3 rescued the effects of BMX downregulation, supporting that BMX signals through STAT3 in glioblastoma stem cells (GSCs). (PMID:21481791)
• This review characterizes the role of BMX in inflamamtion, cardiovascular disease and cancer. (PMID:22449076)
• Overexpression of ETK is associated with the malignancy and disease progression of renal cell carcinoma. (PMID:24606948)
• BMX is an antiapoptotic downstream effector of PI3K, independent of AKT. (PMID:24709422)
• The effects of dietary K(+) on Bmx were more pronounced (PMID:24785188)
• These findings suggested that polymorphisms of the BMX gene could be a potential predictor of clinical symptoms following mTBI. (PMID:24860816)
• Report BMX-ARHGAP gene fusion in gastric cardia adenocarcinoma. (PMID:25499959)
• BMX directly inhibits a core component of the intrinsic apoptosis machinery opens opportunities to improve the efficacy of existing chemotherapy by potentiating BAK-driven cell death in cancer cells. (PMID:25649765)
• Data indicate that EPHA3 is involved in regulating the multidrug resistance (MDR) of small cell lung cancer (SCLC) via PI3K/BMX/STAT3 signaling and may be a therapeutic target in SCLC. (PMID:27101199)
• results demonstrate that cleaved BMX is a novel N-end rule substrate, and its degradation exhibits a novel interplay between substrate phosphorylation and N-end rule degradation, revealing an increasing complex regulatory network of apoptotic proteolytic signaling cascades. (PMID:27601470)
• The studies suggested that BMXDeltaN might play roles in lung tumorigenicity, with expression of BMXDeltaN promoting cell growth, cell migration, and cell transformation. (PMID:28422715)
• These results suggested that BMX can promote cell proliferation through PI3K/AKT/mTOR and STAT3 signaling pathways in cervical cancer cells. (PMID:28514765)
• Epithelial and endothelial tyrosine kinase (Etk) interacts with 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 4 (PFKFB4) to promote small-cell lung cancer (SCLC) chemoresistance through regulation of autophagy. (PMID:29208667)
• results demonstrate that hypoxia-dependent upregulation of BMX contributes to therapeutic resistance through a compensatory prosurvival signaling mechanism. These results also reveal the role of off-target drug effects on tumor microenvironment and development of acquired drug resistance. (PMID:29227282)
• tyrosine kinase BMX is negatively regulated by androgen and contributes to castration-resistant prostate cancer by enhancing the phosphorylation and activation of multiple receptor tyrosine kinases following androgen deprivation therapy (PMID:30012673)
• Linc00173 upregulated Etk through functioning as a competitive endogenous RNA (ceRNA) by “sponging” miRNA-218 and led to the upregulation of GSKIP and NDRG1, resulting in the translocation of beta-catenin. Importantly, expression analysis revealed that both Linc00173 and Etk were upregulated in SCLC patient samples and exhibiting positive Linc00173/Etk correlation (PMID:31477834)
• BMX controls 3betaHSD1 and sex steroid biosynthesis in cancer. (PMID:36647826)
• Preclinical spheroid models identify BMX as a therapeutic target for metastatic MYCN nonamplified neuroblastoma. (PMID:39133652)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Bmx	ENSMUSG00000031377
rattus_norvegicus	Bmx	ENSRNOG00000003705

Paralogs (32): FGR (ENSG00000000938), MATK (ENSG00000007264), BTK (ENSG00000010671), FYN (ENSG00000010810), STYK1 (ENSG00000060140), TNK2 (ENSG00000061938), TXK (ENSG00000074966), JAK2 (ENSG00000096968), ABL1 (ENSG00000097007), PTK6 (ENSG00000101213), HCK (ENSG00000101336), CSK (ENSG00000103653), TYK2 (ENSG00000105397), JAK3 (ENSG00000105639), FRK (ENSG00000111816), ITK (ENSG00000113263), ZAP70 (ENSG00000115085), PTK2B (ENSG00000120899), SRMS (ENSG00000125508), TEC (ENSG00000135605), BLK (ENSG00000136573), ABL2 (ENSG00000143322), FER (ENSG00000151422), JAK1 (ENSG00000162434), SYK (ENSG00000165025), PTK2 (ENSG00000169398), TNK1 (ENSG00000174292), YES1 (ENSG00000176105), FES (ENSG00000182511), LCK (ENSG00000182866), SRC (ENSG00000197122), LYN (ENSG00000254087)

Protein

Protein identifiers

Cytoplasmic tyrosine-protein kinase BMX — P51813 (reviewed: P51813)

Alternative names: Bone marrow tyrosine kinase gene in chromosome X protein, Epithelial and endothelial tyrosine kinase, NTK38

All UniProt accessions (1): P51813

UniProt curated annotations — full annotation on UniProt →

Function. Non-receptor tyrosine kinase that plays central but diverse modulatory roles in various signaling processes involved in the regulation of actin reorganization, cell migration, cell proliferation and survival, cell adhesion, and apoptosis. Participates in signal transduction stimulated by growth factor receptors, cytokine receptors, G-protein coupled receptors, antigen receptors and integrins. Induces tyrosine phosphorylation of BCAR1 in response to integrin regulation. Activation of BMX by integrins is mediated by PTK2/FAK1, a key mediator of integrin signaling events leading to the regulation of actin cytoskeleton and cell motility. Plays a critical role in TNF-induced angiogenesis, and implicated in the signaling of TEK and FLT1 receptors, 2 important receptor families essential for angiogenesis. Required for the phosphorylation and activation of STAT3, a transcription factor involved in cell differentiation. Also involved in interleukin-6 (IL6) induced differentiation. Also plays a role in programming adaptive cytoprotection against extracellular stress in different cell systems, salivary epithelial cells, brain endothelial cells, and dermal fibroblasts. May be involved in regulation of endocytosis through its interaction with an endosomal protein RUFY1. May also play a role in the growth and differentiation of hematopoietic cells; as well as in signal transduction in endocardial and arterial endothelial cells.

Subunit / interactions. Interacts with BCAR1, CAV1, MYD88, PTK2/FAK1, RUFY1, RUFY2, STAT3, TIRAP and TNFRSF1B.

Subcellular location. Cytoplasm.

Tissue specificity. Highly expressed in cells with great migratory potential, including endothelial cells and metastatic carcinoma cell lines.

Post-translational modifications. Phosphorylated in response to protein I/II and to LPS. Phosphorylation at Tyr-566 by SRC and by autocatalysis leads to activation and is required for STAT3 phosphorylation by BMX.

Activity regulation. TEK and vascular endothelial growth factor receptor 1 (FLT1) stimulate BMX tyrosine kinase activity. Activated by integrins through the mediation of PTK2/FAK1. Activated by TNF through the mediation of TNFRSF1B.

Cofactor. Binds 1 zinc ion per subunit.

Domain organisation. SH2 domain mediates interaction with RUFY1.

Induction. Activated by IL6/interleukin-6 through phosphatidylinositol 3-kinase (PI3-kinase) pathway. It is likely that activation occurs through binding of phosphoinositides to the PH domain.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. TEC subfamily.

RefSeq proteins (3): NP_001307795, NP_001712, NP_975010* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR000980	SH2	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR001562	Znf_Btk_motif	Conserved_site
IPR001849	PH_domain	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR011993	PH-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR020635	Tyr_kinase_cat_dom	Domain
IPR035875	BMX_SH2	Domain
IPR036860	SH2_dom_sf	Homologous_superfamily
IPR050198	Non-receptor_tyrosine_kinases	Family

Pfam: PF00017, PF00169, PF00779, PF07714

Enzyme classification (BRENDA):

• EC 2.7.10.2 — non-specific protein-tyrosine kinase (BRENDA: 41 organisms, 396 substrates, 479 inhibitors, 43 Km, 32 kcat entries)

Substrate kinetics (BRENDA)

6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.014–17.64	12
[KDSRC KINASE]-L-TYROSINE	0.0057–0.24	12
POLY(GLU4-TYR)	0.018–0.659	10
EEEEYIQ[DP]-8-HYDROXY-5-(N,N-DIMETHYLSULFONAMIDO	0.057	1
S1 PEPTIDE	0.037	1
EEEEY	—	0

Catalyzed reactions (Rhea), 1 shown:

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)

UniProt features (59 total): strand 18, helix 16, binding site 6, turn 4, domain 3, modified residue 3, sequence variant 2, sequence conflict 2, chain 1, mutagenesis site 1, zinc finger region 1, short sequence motif 1, active site 1

Structure

Experimental structures (PDB)

6 structures.

PDB	Method	Resolution (Å)
8X2A	X-RAY DIFFRACTION	1.3
3SXS	X-RAY DIFFRACTION	1.89
6I99	X-RAY DIFFRACTION	2
3SXR	X-RAY DIFFRACTION	2.4
2EKX	SOLUTION NMR
2YS2	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P51813-F1	76.15	0.45

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 536 (proton acceptor)

Ligand- & substrate-binding residues (6): 143; 423–431; 445; 121; 132; 133

Post-translational modifications (3): 216, 224, 566

Mutagenesis-validated functional residues (1):

Position	Phenotype
566	abolishes almost completely the src-induced phosphorylation of bmx.

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-111465	Apoptotic cleavage of cellular proteins
R-HSA-1660499	Synthesis of PIPs at the plasma membrane
R-HSA-109581	Apoptosis
R-HSA-1430728	Metabolism
R-HSA-1483255	PI Metabolism
R-HSA-1483257	Phospholipid metabolism
R-HSA-5357801	Programmed Cell Death
R-HSA-556833	Metabolism of lipids
R-HSA-75153	Apoptotic execution phase

MSigDB gene sets: 158 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, BENPORATH_ES_WITH_H3K27ME3, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, GOBP_ANTIGEN_RECEPTOR_MEDIATED_SIGNALING_PATHWAY, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOCC_RUFFLE, AAAYRNCTG_UNKNOWN, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, CEBPB_01, GOBP_PHOSPHOLIPID_BIOSYNTHETIC_PROCESS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, YORDY_RECIPROCAL_REGULATION_BY_ETS1_AND_SP100_DN, WEI_MYCN_TARGETS_WITH_E_BOX, GOBP_REGULATION_OF_IMMUNE_RESPONSE

GO Biological Process (10): adaptive immune response (GO:0002250), protein phosphorylation (GO:0006468), phosphatidylinositol biosynthetic process (GO:0006661), apoptotic process (GO:0006915), cell adhesion (GO:0007155), signal transduction (GO:0007165), mesoderm development (GO:0007498), intracellular signal transduction (GO:0035556), B cell receptor signaling pathway (GO:0050853), protein autophosphorylation (GO:0046777)

GO Molecular Function (10): protein tyrosine kinase activity (GO:0004713), non-membrane spanning protein tyrosine kinase activity (GO:0004715), ATP binding (GO:0005524), zinc ion binding (GO:0008270), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), metal ion binding (GO:0046872)

GO Cellular Component (5): nucleoplasm (GO:0005654), cytosol (GO:0005829), plasma membrane (GO:0005886), ruffle membrane (GO:0032587), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Apoptotic execution phase	1
PI Metabolism	1
Programmed Cell Death	1
Phospholipid metabolism	1
Metabolism of lipids	1
Metabolism	1
Apoptosis	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
cellular process	2
intracellular anatomical structure	2
immune response	1
phosphorylation	1
protein modification process	1
biosynthetic process	1
phosphatidylinositol metabolic process	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
cell communication	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
tissue development	1
signal transduction	1
antigen receptor-mediated signaling pathway	1
protein phosphorylation	1
protein kinase activity	1
protein tyrosine kinase activity	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transition metal ion binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
cation binding	1
nuclear lumen	1
cytoplasm	1
membrane	1
cell periphery	1
ruffle	1
cell projection membrane	1
leading edge membrane	1

Protein interactions and networks

STRING

1712 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BMX	STAP1	Q9ULZ2	770
BMX	STAT3	P40763	737
BMX	PLEK2	Q9NYT0	705
BMX	PLEK	P08567	703
BMX	RUFY2	Q8WXA3	524
BMX	KDR	P35968	497
BMX	JAK3	P52333	479
BMX	EGFR	P00533	471
BMX	PFKFB4	Q16877	467
BMX	ERBB4	Q15303	466
BMX	CDC42	P21181	461
BMX	ERBB2	P04626	458
BMX	GJA5	P36382	443
BMX	EFNB2	P52799	440
BMX	TKTL2	Q9H0I9	418

IntAct

52 interactions, top by confidence:

A	B	Type	Score
BMX	STAT3	psi-mi:“MI:0915”(physical association)	0.830
STAT3	BMX	psi-mi:“MI:0915”(physical association)	0.830
BMX	BIRC2	psi-mi:“MI:0915”(physical association)	0.560
BMX	PTPN21	psi-mi:“MI:0915”(physical association)	0.560
BMX	HSP90AB1	psi-mi:“MI:0915”(physical association)	0.560
BMX	PIM1	psi-mi:“MI:0915”(physical association)	0.540
PIM1	BMX	psi-mi:“MI:0915”(physical association)	0.540
PIM1	BMX	psi-mi:“MI:0403”(colocalization)	0.540
BMX	ARIH2	psi-mi:“MI:0914”(association)	0.530
PTPRD	BMX	psi-mi:“MI:0407”(direct interaction)	0.440
	BMX	psi-mi:“MI:0407”(direct interaction)	0.440
BMX	ERBB2	psi-mi:“MI:0407”(direct interaction)	0.440
BMX	EGFR	psi-mi:“MI:0407”(direct interaction)	0.440
BMX	PKM	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
CRK	BMX	psi-mi:“MI:0915”(physical association)	0.400
BMX	YWHAE	psi-mi:“MI:0915”(physical association)	0.400
SFN	BMX	psi-mi:“MI:0915”(physical association)	0.400
BMX	PIM1	psi-mi:“MI:0915”(physical association)	0.400
PIM1	BMX	psi-mi:“MI:0915”(physical association)	0.400
TP53	BMX	psi-mi:“MI:0915”(physical association)	0.400
BMX	CLNK	psi-mi:“MI:0915”(physical association)	0.370
BMX	NOPCHAP1	psi-mi:“MI:0915”(physical association)	0.370
PRDM1	RRAS	psi-mi:“MI:0914”(association)	0.350

BioGRID (103): STAT3 (Two-hybrid), BMX (Reconstituted Complex), BMX (Two-hybrid), BMX (Two-hybrid), STAT3 (Two-hybrid), PTPN21 (Two-hybrid), CC2D1B (Affinity Capture-MS), USP24 (Affinity Capture-MS), ARIH2 (Affinity Capture-MS), BMX (Affinity Capture-MS), WDR45B (Affinity Capture-MS), BMX (Affinity Capture-MS), PDCD2L (Affinity Capture-MS), COPS8 (Affinity Capture-MS), BMX (Reconstituted Complex)

ESM2 similar proteins: A7A1P0, A8WZ92, B4IT27, B5VNQ3, B6A7Q3, C0RW22, F1N9Y5, G5EC24, H2KZW3, O01798, O12990, O19064, O35495, O60674, O94921, P08458, P22517, P23458, P23561, P26818, P27466, P32865, P34635, P34892, P35626, P42159, P42687, P43405, P48025, P51813, P52332, P53356, P83104, Q00537, Q00655, Q09639, Q10056, Q12469, Q17833, Q24145

Diamond homologs: A0A2R6XIK6, A2VDU3, A7J1T0, A7J1T2, A7MBB4, A8X775, D3ZG83, F4JTP5, G5EE56, O01700, O22558, O35346, O43283, O43318, O64768, P08630, P0C8E4, P0CD62, P18106, P18160, P18161, P29317, P32577, P34152, P41239, P41240, P41241, P42680, P42686, P42690, P51813, P80192, P97504, Q00944, Q02779, Q02977, Q03145, Q05397, Q05609, Q0VBZ0

SIGNOR signaling

16 interactions.

A	Effect	B	Mechanism
BMX	up-regulates	PTK2	phosphorylation
TEC	“up-regulates activity”	BMX	phosphorylation
BMX	“up-regulates activity”	STAT3	phosphorylation
BMX	“down-regulates activity”	F2R	phosphorylation
SRC	up-regulates	BMX	phosphorylation
BTK	up-regulates	BMX	phosphorylation
TEC	up-regulates	BMX	phosphorylation
BMX	“up-regulates quantity”	BCAR1	phosphorylation
ITK	“up-regulates activity”	BMX	phosphorylation
PTPRG	“down-regulates activity”	BMX	dephosphorylation
9-(1-Methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone	“down-regulates activity”	BMX	“chemical inhibition”
BMX	“up-regulates activity”	RUFY1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 31 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Cytokine Signaling in Immune system	6	10.6×	1e-03
Signaling by Rho GTPases	5	7.4×	7e-03
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	5	7.3×	7e-03

GO biological processes:

GO term	Partners	Fold	FDR
regulation of cell cycle	5	13.3×	5e-03
cell surface receptor signaling pathway	5	11.4×	6e-03
negative regulation of apoptotic process	9	11.2×	4e-05
positive regulation of gene expression	6	8.3×	6e-03
intracellular signal transduction	6	8.2×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

46 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	14
Likely benign	0
Benign	1

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
688137	GRCh37/hg19 Xp22.33-q28(chrX:168546-155233731)x1	Pathogenic

SpliceAI

3031 predictions. Top by Δscore:

Variant	Effect	Δscore
X:15479723:ACTT:A	donor_loss	1.0000
X:15479725:TTACT:T	donor_loss	1.0000
X:15479726:TACT:T	donor_loss	1.0000
X:15479727:A:AC	donor_gain	1.0000
X:15479728:C:CT	donor_gain	1.0000
X:15479728:CT:C	donor_gain	1.0000
X:15479728:CTG:C	donor_gain	1.0000
X:15479728:CTGT:C	donor_gain	1.0000
X:15479728:CTGTT:C	donor_gain	1.0000
X:15479817:TTTAA:T	acceptor_gain	1.0000
X:15479818:TTAA:T	acceptor_gain	1.0000
X:15479819:TAA:T	acceptor_gain	1.0000
X:15479819:TAAC:T	acceptor_loss	1.0000
X:15479820:AA:A	acceptor_gain	1.0000
X:15479820:AAC:A	acceptor_loss	1.0000
X:15479822:C:CC	acceptor_gain	1.0000
X:15479822:C:T	acceptor_loss	1.0000
X:15479823:T:A	acceptor_loss	1.0000
X:15493188:A:AC	donor_gain	1.0000
X:15493189:C:CC	donor_gain	1.0000
X:15493189:CG:C	donor_gain	1.0000
X:15493189:CGCTG:C	donor_gain	1.0000
X:15508340:TTTA:T	acceptor_loss	1.0000
X:15508342:TA:T	acceptor_loss	1.0000
X:15508343:A:AG	acceptor_gain	1.0000
X:15508343:AGG:A	acceptor_loss	1.0000
X:15508343:AGGAT:A	acceptor_gain	1.0000
X:15508344:G:GG	acceptor_gain	1.0000
X:15508344:GGAT:G	acceptor_gain	1.0000
X:15508344:GGATG:G	acceptor_gain	1.0000

AlphaMissense

4476 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:15531343:T:C	F319L	1.000
X:15531345:T:A	F319L	1.000
X:15531345:T:G	F319L	1.000
X:15534310:T:C	L373P	1.000
X:15537246:G:C	K445N	1.000
X:15537246:G:T	K445N	1.000
X:15542191:G:C	R535P	1.000
X:15542194:A:C	D536A	1.000
X:15542194:A:G	D536G	1.000
X:15542194:A:T	D536V	1.000
X:15543120:A:T	D554V	1.000
X:15543121:C:A	D554E	1.000
X:15543121:C:G	D554E	1.000
X:15546858:T:A	W578R	1.000
X:15546858:T:C	W578R	1.000
X:15546860:G:C	W578C	1.000
X:15546860:G:T	W578C	1.000
X:15546912:T:A	W596R	1.000
X:15546912:T:C	W596R	1.000
X:15549989:T:A	W649R	1.000
X:15549989:T:C	W649R	1.000
X:15556085:C:A	R656S	1.000
X:15508385:T:C	L11P	0.999
X:15508392:A:C	K13N	0.999
X:15508392:A:T	K13N	0.999
X:15508439:G:C	R29P	0.999
X:15508445:T:C	F31S	0.999
X:15508466:T:C	L38P	0.999
X:15511459:T:C	L89P	0.999
X:15511497:T:A	W102R	0.999

dbSNP variants (sampled 300 via entrez): RS1000009210 (X:15527253 T>C,G), RS1000064566 (X:15501225 G>A), RS1000216366 (X:15544003 C>G,T), RS1000257980 (X:15514282 C>T), RS1000283132 (X:15500852 T>A,C), RS1000332058 (X:15525745 G>A), RS1000366511 (X:15526150 T>A,G), RS1000510959 (X:15551215 T>C), RS1000548845 (X:15541278 G>A,C), RS1000813309 (X:15550788 A>G), RS1000887626 (X:15505527 G>T), RS1001056243 (X:15538438 G>A), RS1001119823 (X:15515763 T>G), RS1001172544 (X:15545688 C>T), RS1001202791 (X:15551130 G>A)

Disease associations

OMIM: gene MIM:300101 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3834 (SINGLE PROTEIN), CHEMBL4296642 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

33 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 69,289 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1834657	INFIGRATINIB PHOSPHATE	4	285
CHEMBL1852688	INFIGRATINIB	4	2,209
CHEMBL1873475	IBRUTINIB	4	7,994
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL3707348	ACALABRUTINIB	4	4,504
CHEMBL3936761	ZANUBRUTINIB	4	2,484
CHEMBL4071161	TIRABRUTINIB	4	2,170
CHEMBL4085457	RITLECITINIB	4	708
CHEMBL5416410	DASATINIB	4	655
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL31965	CANERTINIB	3	8,083
CHEMBL3702854	RILZABRUTINIB	3	851
CHEMBL4072833	EVOBRUTINIB	3	960
CHEMBL4483575	REMIBRUTINIB	3	569
CHEMBL603469	LESTAURTINIB	3
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL1738757	REBASTINIB	2	1,478
CHEMBL3301625	SPEBRUTINIB	2	2,965
CHEMBL3900554	BMS-986142	2	66
CHEMBL4094440	BMS-919373	2
CHEMBL4114766	ATUZABRUTINIB	2
CHEMBL4297674	BRANEBRUTINIB	2
CHEMBL44	GENISTEIN	2
CHEMBL475251	R-406	2
CHEMBL5077961	MILREBRUTINIB	2
CHEMBL5083772	BIIB-091	2
CHEMBL572878	TOZASERTIB	2
CHEMBL607707	PELITINIB	2
CHEMBL1908397	KW-2449	1

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Tec family

Most potent curated ligand interactions (11 total), top 11:

Ligand	Action	Affinity	Parameter
compound 38 [PMID: 24915291]	Inhibition	9.15	pIC50
ibrutinib	Inhibition	9.1	pIC50
compound 31 [PMID: 24915291]	Inhibition	8.72	pIC50
nemtabrutinib	Inhibition	8.28	pIC50
compound 9 [PMID: 26006010]	Inhibition	8.12	pIC50
BMX-IN-1	Inhibition	8.1	pIC50
PRN694	Inhibition	7.77	pIC50
acalabrutinib	Inhibition	7.34	pIC50
BIIB091	Inhibition	7.06	pKd
ZYBT1	Inhibition	7.04	pIC50
JNJ-64264681	Inhibition	6.76	pIC50

Binding affinities (BindingDB)

82 measured of 106 human assays (106 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one	IC50	0.8 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
IBRUTINIB	IC50	0.8 nM	US-9278100: Inhibitors of bruton’s tyrosine kinase for the treatment of solid tumors
N-[4-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]cyclohexyl]prop-2-enamide	IC50	1.1 nM	US-9278100: Inhibitors of bruton’s tyrosine kinase for the treatment of solid tumors
1-[(3R)-3-[[2-(2,5,8,11-tetraoxabicyclo[10.4.0]hexadeca-1(12),13,15-trien-14-ylamino)-7H-purin-6-yl]amino]piperidin-1-yl]prop-2-en-1-one	IC50	1.69 nM	US-11440904: Substituted pyrimidines, pharmaceutical compositions and therapeutic methods thereof
Staurosporine	KD	1.7 nM
N-[3-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-4-propan-2-yloxycyclohexa-2,4-dien-1-yl]-1H-pyrazole-4-carboxamide	IC50	2.2 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
AVL-292	IC50	3.2 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
QL-XII-44	IC50	5.62 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
9-(1-methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-one	IC50	6.73 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-X-138	IC50	7 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,	IC50	7.99 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(3-cyclopropylphenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	8 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
QL-XII-56	IC50	8 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-46	IC50	8.75 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
N-[3-[2-[4-amino-1-(4-hydroxycyclohexyl)pyrazolo[3,4-d]pyrimidin-3-yl]ethynyl]-4-methylphenyl]-4-methyl-3-(trifluoromethyl)benzamide	IC50	10 nM	US-10266537: 3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
QL-XI-13	IC50	10.5 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
tert-butyl 4-amino-3-[2-[2-methyl-5-[[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]phenyl]ethynyl]pyrazolo[3,4-d]pyrimidine-1-carboxylate	IC50	11 nM	US-10266537: 3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
QL-XI-76	IC50	12 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-X-134	IC50	12.9 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-115	IC50	13 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-45	IC50	13 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-X-132	IC50	15.7 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XI-77	IC50	15.9 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(3-chlorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	16 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	17 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
N-[3-[2-[4-amino-1-(1-methylpiperidin-4-yl)pyrazolo[3,4-d]pyrimidin-3-yl]ethynyl]-4-methylphenyl]-3-(trifluoromethyl)benzamide	IC50	18 nM	US-10266537: 3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
QL-XII-51	IC50	18 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-58	IC50	18.1 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-54	IC50	18.5 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
1-[(3R)-3-[[2-(2,5,8,11-tetraoxabicyclo[10.4.0]hexadeca-1(12),13,15-trien-14-ylamino)-7H-purin-6-yl]amino]piperidin-1-yl]propan-1-one	IC50	19.6 nM	US-11440904: Substituted pyrimidines, pharmaceutical compositions and therapeutic methods thereof
QL-XI-75	IC50	19.7 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[2-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	21 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
3-[2-[4-amino-1-(1-prop-2-enoylpiperidin-4-yl)pyrazolo[3,4-d]pyrimidin-3-yl]ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide	IC50	22 nM	US-10266537: 3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
5-amino-3-(1-benzylpyrazol-4-yl)-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)pyrazole-4-carboxamide	IC50	24 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[2-fluoro-3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	25 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
BMS-354825	KD	27 nM
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2-chlorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	27 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2-fluorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	27 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
QL-XII-66	IC50	27.8 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	29 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	33 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide	IC50	33 nM
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2-chloro-3-fluorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	34 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2-chloro-5-fluorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	35 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2-cyanophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	37 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[3-(difluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	37 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[(2,3-difluorophenyl)methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	38 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors
QL-XII-37	IC50	40.6 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
QL-XII-63	IC50	41 nM	US-10000483: Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
5-amino-1-(6-but-2-ynoyl-6-azaspiro[3.4]octan-2-yl)-3-[1-[[4-chloro-3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]pyrazole-4-carboxamide	IC50	46 nM	US-9975882: Heteroaromatic compounds as BTK inhibitors

ChEMBL bioactivities

437 potent at pChembl≥5 of 449 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.40	IC50	0.4	nM	IBRUTINIB
9.40	IC50	0.4	nM	CHEMBL3647964
9.40	IC50	0.4	nM	CHEMBL1643976
9.39	IC50	0.41	nM	CHEMBL5757288
9.30	IC50	0.5	nM	IBRUTINIB
9.22	IC50	0.6	nM	CHEMBL5189379
9.21	IC50	0.62	nM	ZANUBRUTINIB
9.15	IC50	0.71	nM	CHEMBL3290148
9.10	IC50	0.8	nM	IBRUTINIB
9.10	IC50	0.8	nM	CHEMBL3182647
9.05	IC50	0.9	nM	CHEMBL4560385
9.05	IC50	0.9	nM	IBRUTINIB
9.00	IC50	1	nM	BOSUTINIB
9.00	IC50	1	nM	IBRUTINIB
9.00	IC50	1	nM	RILZABRUTINIB
8.96	IC50	1.1	nM	CHEMBL3647967
8.96	IC50	1.1	nM	CHEMBL5188812
8.92	IC50	1.2	nM	CHEMBL5271284
8.92	IC50	1.21	nM	CHEMBL5903840
8.89	IC50	1.3	nM	CHEMBL3932338
8.85	IC50	1.4	nM	CHEMBL459850
8.85	IC50	1.4	nM	CHEMBL5193128
8.85	Kd	1.4	nM	IBRUTINIB
8.85	Kd	1.4	nM	DASATINIB
8.82	IC50	1.5	nM	BRANEBRUTINIB
8.81	IC50	1.53	nM	CHEMBL1916891
8.80	Kd	1.6	nM	IBRUTINIB
8.77	IC50	1.69	nM	CHEMBL5999061
8.74	IC50	1.8	nM	ATUZABRUTINIB
8.72	IC50	1.9	nM	CHEMBL3290142
8.72	IC50	1.9	nM	CHEMBL6055510
8.66	IC50	2.2	nM	CHEMBL5872185
8.62	IC50	2.4	nM	CHEMBL5853650
8.60	IC50	2.5	nM	CHEMBL5404368
8.57	IC50	2.7	nM	CHEMBL5786294
8.54	IC50	2.9	nM	CHEMBL5760493
8.54	IC50	2.9	nM	CHEMBL6000385
8.52	IC50	2.99	nM	STAUROSPORINE
8.52	IC50	3	nM	CHEMBL6009940
8.51	IC50	3.1	nM	CHEMBL5989466
8.49	IC50	3.2	nM	SPEBRUTINIB
8.48	IC50	3.3	nM	CHEMBL4248386
8.46	IC50	3.5	nM	CHEMBL4568087
8.46	IC50	3.5	nM	CHEMBL5912796
8.42	IC50	3.8	nM	CHEMBL4752700
8.38	IC50	4.2	nM	CHEMBL5915958
8.37	IC50	4.3	nM	TIRABRUTINIB
8.35	IC50	4.5	nM	CHEMBL6043477
8.28	IC50	5.2	nM	CHEMBL4241958
8.28	IC50	5.29	nM	STAUROSPORINE

PubChem BioAssay actives

281 with measured affinity, of 1183 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
1-[(3S)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one	1784109: Inhibition of N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	ic50	0.0004	uM
Ibrutinib	1781997: Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	ic50	0.0004	uM
N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide	2185102: Inhibition of TEL fused BMX (unknown origin) transformed in mouse BaF3 cells	ic50	0.0004	uM
Ritlecitinib	1802326: TR-FRET Competition Assay from Article 10.1021/acschembio.6b00677: “Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.”	ki	0.0005	uM
Zanubrutinib	1615368: Inhibition of human BMX using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method	ic50	0.0006	uM
(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-(4-methylpiperazin-1-yl)pent-2-enenitrile	1850189: Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method	ic50	0.0006	uM
2-methyl-N-[2-[3-[[2-(prop-2-enoylamino)acetyl]amino]anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide	1155542: Inhibition of Bmx (unknown origin) after 1 hr by HTRF assay	ic50	0.0007	uM
5-amino-1-[(3R)-1-cyanopiperidin-3-yl]-3-[4-(2,4-difluorophenoxy)phenyl]pyrazole-4-carboxamide	1940004: Inhibition of BMX (unknown origin)	ic50	0.0009	uM
Bosutinib	1301436: Inhibition of human BMX using poly(Glu,Tyr) 4:1 as substrate after 40 mins by scintillation counting analysis in presence of [gamma-33P-ATP]	ic50	0.0010	uM
(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile	1850252: Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP	ic50	0.0010	uM
N-[3-[3-(prop-2-enoylamino)phenyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]thiophene-2-carboxamide	1872699: Inhibition of BMX (unknown origin)	ic50	0.0011	uM
1-[(3S)-3-[4-amino-3-(2-methyl-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one	1954478: Inhibition of BMX (unknown origin) by Z’LYTE assay	ic50	0.0012	uM
(7S)-7-(1-but-2-ynoylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide	1948231: Inhibition of human BMX preincubated for 1 hrs followed by substrate addition and measured after 1 hrs in the presence of ATP at Km concentration by TR-FRET assay	ic50	0.0013	uM
N-[3-(7-amino-1-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl)-4-methylphenyl]-3-(trifluoromethyl)benzamide	383099: Inhibition of Bmx	ic50	0.0014	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate	435781: Binding constant for full-length BMX	kd	0.0014	uM
(7S)-2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-3,3a,4,5,6,7-hexahydropyrazolo[1,5-a]pyrimidine-3-carboxamide	1871764: Inhibition of BMX (unknown origin)	ic50	0.0014	uM
4-[(3S)-3-(but-2-ynoylamino)piperidin-1-yl]-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide	1656253: Inhibition of BMX (unknown origin)	ic50	0.0015	uM
(E)-4-(dimethylamino)-N-[7-fluoro-4-(2-methylanilino)imidazo[1,5-a]quinoxalin-8-yl]-N-methylbut-2-enamide	629923: Inhibition of BMX relative to control	ic50	0.0015	uM
(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile	1850189: Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method	ic50	0.0018	uM
2-methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide	1155542: Inhibition of Bmx (unknown origin) after 1 hr by HTRF assay	ic50	0.0019	uM
1-[(3R)-3-[5-(4-phenoxyanilino)-2,6,7,9,11-pentazatricyclo[6.3.1.04,12]dodeca-1,3,5,8(12),9-pentaen-7-yl]pyrrolidin-1-yl]prop-2-en-1-one	2001966: Inhibition of BMX (unknown origin) by filter binding method	ic50	0.0025	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	1715441: Inhibition of human BMX using polyGlu:Tyr as substrate by [gamma-33P]-ATP assay	ic50	0.0030	uM
4-[3-(ethenylsulfonylamino)-2-methylphenyl]-2,3-dimethyl-1H-indole-7-carboxamide	1399232: Inhibition of BMX (unknown origin)	ic50	0.0033	uM
N-[(1R,2S)-2-aminocyclohexyl]-4-[6-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]thiophene-2-carboxamide	1637055: Inhibition of full-length recombinant human His-tagged BMX expressed in baculovirus expression system by Z’-LYTE assay	ic50	0.0035	uM
N-(4-ethyl-2-pyridinyl)-4-[6-(prop-2-enoylamino)quinolin-4-yl]oxybenzamide	1720523: Inhibition of His-tagged recombinant full length human His-tagged BMX cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z’-LYTE assay	ic50	0.0038	uM
6-amino-9-[(3R)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one	1871764: Inhibition of BMX (unknown origin)	ic50	0.0043	uM
7-(2-hydroxypropan-2-yl)-4-[2-methyl-3-(prop-2-enoylamino)phenyl]-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamide	1399232: Inhibition of BMX (unknown origin)	ic50	0.0052	uM
1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0056	uM
4-[3-[(6R,8aS)-1,1-dimethyl-3-oxo-6,7,8,8a-tetrahydro-5H-[1,3]oxazolo[3,4-a]pyridin-6-yl]-8-aminoimidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)-2-pyridinyl]benzamide	1721748: Inhibition of BMX (unknown origin)	ic50	0.0056	uM
1-[(3S)-3-[4-amino-3-(2,6-dimethyl-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one	1954478: Inhibition of BMX (unknown origin) by Z’LYTE assay	ic50	0.0057	uM
4-(methylamino)-2-[4-methyl-3-(prop-2-enoylamino)anilino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]pyrimidine-5-carboxamide	1440723: Irreversible inhibition of inactive state of wild-type full-length recombinant His-tagged BMX phosphorylation (unknown origin) at tyrosine residue expressed in baculovirus infected SF9 cells preincubated for 30 mins followed by ATP addition measured after 20 mins by Western blot analysis	ec50	0.0058	uM
9-(1-methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-one	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0067	uM
3-chloro-4-[3-(5-chloro-1,3-dioxopyrido[1,2-c]pyrimidin-2-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide	1678394: Inhibition of BMX (unknown origin)	ic50	0.0070	uM
N-[2-methyl-5-[2-oxo-9-(1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-1-yl]phenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0074	uM
N-[4-methyl-3-[1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide	1440720: Inhibition of full-length recombinant human His-tagged BMX expressed in baculovirus expression system using Poly(4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay	ic50	0.0080	uM
N-[4-methyl-3-[1-methyl-7-[4-methyl-3-(prop-2-enoylamino)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide	1440720: Inhibition of full-length recombinant human His-tagged BMX expressed in baculovirus expression system using Poly(4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay	ic50	0.0080	uM
N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0080	uM
N-[2-methyl-5-[9-(1-methylpyrazol-4-yl)-2-oxobenzo[h][1,6]naphthyridin-1-yl]phenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0082	uM
2-[3-[2-amino-6-[1-(oxetan-3-yl)-3,6-dihydro-2H-pyridin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one	1830223: Inhibition of human full-length BMX (1 to 675 residues) expressed in baculovirus expression system by mobility shift assay	ic50	0.0085	uM
1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)-9-(1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-2-one	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0088	uM
(Z)-2-[(2R)-2-[[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]pyrrolidine-1-carbonyl]-4-methyl-4-morpholin-4-ylpent-2-enenitrile	1850189: Inhibition of BMX (unknown origin) using peptide substrate in presence of ATP by caliper electrophoresis method	ic50	0.0101	uM
N-[3-[2-oxo-9-(1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-1-yl]phenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0105	uM
4-[8-amino-3-[(3R,6S)-1-(cyclopropanecarbonyl)-6-methylpiperidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)-2-pyridinyl]benzamide	1711654: Inhibition of human BMX	ic50	0.0110	uM
4-[8-amino-3-[(6R,8aS)-3-oxo-2,5,6,7,8,8a-hexahydro-1H-indolizin-6-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)-2-pyridinyl]benzamide	1721748: Inhibition of BMX (unknown origin)	ic50	0.0110	uM
3-amino-5-[4-[[4-(4-chlorophenyl)-2-pyridinyl]carbamoyl]phenyl]-2-[(2S)-1-prop-2-enoylpiperidin-2-yl]imidazole-4-carboxamide	1781997: Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA	ic50	0.0113	uM
4-[7-methoxy-6-(5-morpholin-4-ylpent-2-ynoylamino)quinolin-4-yl]oxy-N-pyridin-2-ylbenzamide	1720523: Inhibition of His-tagged recombinant full length human His-tagged BMX cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z’-LYTE assay	ic50	0.0120	uM
N-[5-[9-(furan-3-yl)-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0121	uM
N-[5-[9-(6-amino-3-pyridinyl)-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide	1499223: Inhibition of recombinant full length His-tagged human BMX expressed in baculovirus expression system using poly (4:1 Glu, Tyr) as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ADP-glo assay	ic50	0.0129	uM
2,3-dimethyl-4-[2-methyl-3-(prop-2-enoylamino)phenyl]-1H-indole-7-carboxamide	1399232: Inhibition of BMX (unknown origin)	ic50	0.0130	uM
4-[8-amino-3-[(6R,8aS)-3-oxo-1,5,6,7,8,8a-hexahydro-[1,3]oxazolo[3,4-a]pyridin-6-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)-2-pyridinyl]benzamide	1721748: Inhibition of BMX (unknown origin)	ic50	0.0130	uM

CTD chemical–gene interactions

23 total (human), top 23 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
cobaltous chloride	decreases expression	1
epigallocatechin gallate	increases expression	1
CGP 52608	affects binding, increases reaction	1
ponatinib	decreases activity	1
Norethindrone Acetate	affects cotreatment, increases expression	1
Acetaminophen	decreases expression	1
Cadmium	increases abundance, increases expression	1
Copper	affects binding, increases expression	1
Doxorubicin	affects response to substance	1
Estradiol	affects cotreatment, increases expression	1
Omeprazole	affects reaction, increases activity	1
Tetrachlorodibenzodioxin	increases expression	1
Thiosemicarbazones	affects binding, increases expression	1
Tobacco Smoke Pollution	increases expression	1
Tretinoin	increases expression	1
Valproic Acid	decreases methylation	1
Vanadium	decreases expression	1
Cyclosporine	increases methylation	1
Antirheumatic Agents	increases expression	1
Cadmium Chloride	increases abundance, increases expression	1
Copper Sulfate	increases expression	1
Nanotubes, Carbon	decreases expression	1
Coal Ash	decreases expression	1

ChEMBL screening assays

504 unique, capped per target: 488 binding, 11 functional, 5 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1006344	Binding	Inhibition of Tel-fused Bmx kinase-mediated mouse BaF3 cell proliferation	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. — Proc Natl Acad Sci U S A
CHEMBL1963769	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: BMX	PubChem BioAssay data set
CHEMBL4023729	ADMET	Inhibition of cytoplasmic recombinant human full length His-tagged BMX expressed in baculovirus at 1 uM by Z’-LYTE assay	Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development. — J Med Chem

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.