CDC42BPA

Summary

CDC42BPA (CDC42 binding protein kinase alpha, HGNC:1737) is a protein-coding gene on chromosome 1q42.13, encoding Serine/threonine-protein kinase MRCK alpha (Q5VT25). Serine/threonine-protein kinase which is an important downstream effector of CDC42 and plays a role in the regulation of cytoskeleton reorganization and cell migration.

The protein encoded by this gene is a member of the serine/threonine protein kinase family. This kinase contains multiple functional domains. Its kinase domain is highly similar to that of the myotonic dystrophy protein kinase (DMPK). This kinase also contains a Rac interactive binding (CRIB) domain, and has been shown to bind CDC42. It may function as a CDC42 downstream effector mediating CDC42 induced peripheral actin formation, and promoting cytoskeletal reorganization. Multiple alternatively spliced transcript variants have been described.

Source: NCBI Gene 8476 — RefSeq curated summary.

At a glance

• GWAS associations: 24
• Clinical variants (ClinVar): 234 total
• Druggable target: yes — 13 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001394014

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1737
Approved symbol	CDC42BPA
Name	CDC42 binding protein kinase alpha
Location	1q42.13
Locus type	gene with protein product
Status	Approved
Aliases	MRCKA, PK428, FLJ23347, KIAA0451, MRCKalpha
Ensembl gene	ENSG00000143776
Ensembl biotype	protein_coding
OMIM	603412
Entrez	8476

Gene structure

Transcript identifiers

Ensembl transcripts: 18 — 12 protein_coding, 5 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000334218, ENST00000366764, ENST00000366766, ENST00000366767, ENST00000366769, ENST00000429440, ENST00000441725, ENST00000442054, ENST00000448940, ENST00000462553, ENST00000466538, ENST00000478573, ENST00000488131, ENST00000682551, ENST00000684580, ENST00000963196, ENST00000963197, ENST00000963198

RefSeq mRNA: 7 — MANE Select: NM_001394014 NM_001366010, NM_001366011, NM_001366019, NM_001387550, NM_001394014, NM_003607, NM_014826

CCDS: CCDS1558, CCDS1559, CCDS91168, CCDS91169, CCDS91170

Canonical transcript exons

ENST00000366766 — 37 exons

Exon	Start	End
ENSE00000961918	227026055	227026152
ENSE00001015669	227033334	227033415
ENSE00001071170	227035471	227035607
ENSE00001145213	227091886	227091991
ENSE00001211868	227034655	227034794
ENSE00001211986	227069777	227069853
ENSE00001289505	227028657	227029250
ENSE00001367385	227047927	227048010
ENSE00001373065	227030408	227030470
ENSE00001378802	227040131	227040236
ENSE00001381144	227031298	227031514
ENSE00001442573	227051881	227051985
ENSE00001879316	226989865	226994399
ENSE00002206005	227317005	227318492
ENSE00002400117	227004994	227005111
ENSE00002419086	227016927	227017050
ENSE00002426973	226994823	226994980
ENSE00002429768	227016080	227016197
ENSE00003510454	227213136	227213219
ENSE00003537828	227074259	227074364
ENSE00003563828	227199557	227199652
ENSE00003596523	227080893	227081017
ENSE00003643494	227254064	227254155
ENSE00003676176	227073864	227074012
ENSE00003693306	227072208	227072299
ENSE00003715485	227112671	227112913
ENSE00003718123	227139576	227139742
ENSE00003721605	227193786	227193934
ENSE00003722449	227142945	227143024
ENSE00003726813	227112312	227112422
ENSE00003737773	227100992	227101239
ENSE00003737849	227160543	227160636
ENSE00003739132	227129109	227129231
ENSE00003746876	227147359	227147559
ENSE00003749556	227119804	227119937
ENSE00003753689	227145489	227145737
ENSE00003786204	227023263	227023347

Expression profiles

Bgee: expression breadth ubiquitous, 291 present calls, max score 98.71.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 19.3323 / max 759.8381, expressed in 1690 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
17798	9.5842	1593
17797	2.9013	1243
17796	2.0996	1068
17795	1.8180	785
17791	1.5559	759
17789	0.8385	351
17786	0.2759	102
17793	0.1538	74
17792	0.0893	30
17794	0.0157	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
medial globus pallidus	UBERON:0002477	98.71	gold quality
globus pallidus	UBERON:0001875	98.50	gold quality
pylorus	UBERON:0001166	98.39	gold quality
tibia	UBERON:0000979	98.23	gold quality
secondary oocyte	CL:0000655	98.06	gold quality
lateral nuclear group of thalamus	UBERON:0002736	98.06	gold quality
lateral globus pallidus	UBERON:0002476	97.84	gold quality
substantia nigra pars reticulata	UBERON:0001966	97.65	gold quality
renal medulla	UBERON:0000362	97.52	gold quality
Brodmann (1909) area 23	UBERON:0013554	97.44	gold quality
corpus callosum	UBERON:0002336	97.40	gold quality
substantia nigra pars compacta	UBERON:0001965	97.31	gold quality
inferior vagus X ganglion	UBERON:0005363	97.26	gold quality
cardia of stomach	UBERON:0001162	96.87	gold quality
visceral pleura	UBERON:0002401	96.81	gold quality
postcentral gyrus	UBERON:0002581	96.81	gold quality
parietal lobe	UBERON:0001872	96.51	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	96.50	gold quality
cerebellar vermis	UBERON:0004720	96.48	gold quality
ventral tegmental area	UBERON:0002691	96.47	gold quality
tendon of biceps brachii	UBERON:0008188	96.44	gold quality
pons	UBERON:0000988	96.09	gold quality
urethra	UBERON:0000057	96.02	gold quality
cranial nerve II	UBERON:0000941	95.97	gold quality
tendon	UBERON:0000043	95.88	gold quality
oocyte	CL:0000023	95.78	gold quality
dorsal root ganglion	UBERON:0000044	95.55	gold quality
occipital lobe	UBERON:0002021	95.26	gold quality
medulla oblongata	UBERON:0001896	95.24	gold quality
dorsal plus ventral thalamus	UBERON:0001897	95.15	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-CURD-119	yes	10.66
E-ANND-3	yes	10.08

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): TP53

miRNA regulators (miRDB)

190 targeting CDC42BPA, 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-3163	100.00	77.23	8605
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-6888-3P	99.97	65.95	1170
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-4666A-3P	99.96	71.71	3434
HSA-MIR-590-3P	99.96	74.34	6478

Literature-anchored findings (GeneRIF, showing 22)

• Class II histone deacetylases are directly recruited by BCL6 transcriptional repressor (PMID:11929873)
• a Cdc42-MRCK signal mediates myosin-dependent cell motility and there is convergence between Rho and Cdc42 signalling (PMID:15723050)
• The level of MRCKalpha mRNA in various tissues strongly positively correlates with the level of TfR mRNA, indicating its possible role in the transferrin iron uptake pathway. (PMID:16412980)
• findings report that the Notch1 gene is a p53 target in human keratinocytes with a role in tumor suppression of this cell type through negative regulation of the ROCK1/2 and MRCKalpha kinases (PMID:17344417)
• analysis of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta (PMID:18263588)
• MRCKalpha takes part in transferrin (Tf)-iron uptake, probably via regulation of Tf- TfR endocytosis/endosome trafficking that is dependent on the cellular cytoskeleton. (PMID:20188707)
• Data show that chelerythrine blocks cellular activity of MRCK resulted in the specific loss of NM II-associated MLC phosphorylation in the lamella, and the consequential suppression of cell migration. (PMID:21457715)
• MRCK participates in mediating the effects of HMI-1a3 on HeLa cell morphology. (PMID:24486483)
• A functional pathway involving PDK1-mediated activation of MRCKA, links EGF signaling to myosin contraction and directional migration. (PMID:25092657)
• the functional relevance of the LRAP25-MRCK complex in LIMK1-cofilin signaling and the importance of LRAP adaptors as key determinants of MRCK cellular localization and downstream specificities. (PMID:25107909)
• Data show that the fusion gene cyclin D1/myotonic dystrophy kinase-related CDC42-binding protein kinase alpha (CCND1/MRCK) mRNA is resistant to CCND1-targeted miRNA regulation. (PMID:27025456)
• ICAP-1 monoubiquitylation helps in switching from ROCK2-mediated to MRCKalpha-mediated cell contractility. (PMID:28049720)
• Silencing of CDC42BPA expression partially reduces miR29a3p inhibitor-induced migration and invasion of SW4807 cells (PMID:29039592)
• Cdc42BPA and Cdc42 signaling are important for colon cancer invasion, and Cdc42BPA has potential implications for colon cancer prognosis and treatment. (PMID:29072916)
• The authors describe the discovery of MRCKalpha as a downstream effector of apoptosis and trigger of epithelial extrusion. By describing this novel role of MRCKalpha during apoptosis, the authors cast light on the complex actomyosin cytoskeleton dynamics in the process of epithelial cell extrusion and, likely, in the homeostatic maintenance of tissues in multicellular organisms. (PMID:29162624)
• Functional proteomics interrogation of the kinome identifies MRCKA as a therapeutic target in high-grade serous ovarian carcinoma. (PMID:32071169)
• Myotonic dystrophy kinase-related CDC42-binding kinase alpha, a new transferrin receptor type 2-binding partner, is a regulator of erythropoiesis. (PMID:33476437)
• The Na+, K+-ATPase beta1 subunit regulates epithelial tight junctions via MRCKalpha. (PMID:33507884)
• Effect and in silico characterization of genetic variants associated with severe spermatogenic disorders in a large Iberian cohort. (PMID:33784440)
• Gene transfer of MRCKalpha rescues lipopolysaccharide-induced acute lung injury by restoring alveolar capillary barrier function. (PMID:34675326)
• MRCK-Alpha and Its Effector Myosin II Regulatory Light Chain Bind ABCB4 and Regulate Its Membrane Expression. (PMID:35203270)
• Tumor-associated macrophage-induced circMRCKalpha encodes a peptide to promote glycolysis and progression in hepatocellular carcinoma. (PMID:38642609)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	cdc42bpab	ENSDARG00000016464
danio_rerio	cdc42bpaa	ENSDARG00000104283
mus_musculus	Cdc42bpa	ENSMUSG00000026490
rattus_norvegicus	Cdc42bpa	ENSRNOG00000002841
drosophila_melanogaster	gek	FBGN0023081
caenorhabditis_elegans		WBGENE00006437

Paralogs (5): ROCK1 (ENSG00000067900), CIT (ENSG00000122966), ROCK2 (ENSG00000134318), CDC42BPG (ENSG00000171219), CDC42BPB (ENSG00000198752)

Protein

Protein identifiers

Serine/threonine-protein kinase MRCK alpha — Q5VT25 (reviewed: Q5VT25)

Alternative names: CDC42-binding protein kinase alpha, DMPK-like alpha, Myotonic dystrophy kinase-related CDC42-binding kinase alpha

All UniProt accessions (7): Q5VT25, A0A0A0MRJ0, A0A0A0MRJ1, A0A8I5QJM2, H0Y5V1, H0Y6R0, H0Y7V8

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine-protein kinase which is an important downstream effector of CDC42 and plays a role in the regulation of cytoskeleton reorganization and cell migration. Regulates actin cytoskeletal reorganization via phosphorylation of PPP1R12C and MYL9/MLC2. In concert with MYO18A and LURAP1, is involved in modulating lamellar actomyosin retrograde flow that is crucial to cell protrusion and migration. Phosphorylates: PPP1R12A, LIMK1 and LIMK2. May play a role in TFRC-mediated iron uptake. In concert with FAM89B/LRAP25 mediates the targeting of LIMK1 to the lamellipodium resulting in its activation and subsequent phosphorylation of CFL1 which is important for lamellipodial F-actin regulation. Triggers the formation of an extrusion apical actin ring required for epithelial extrusion of apoptotic cells.

Subunit / interactions. Homodimer and homotetramer via the coiled coil regions. Interacts tightly with GTP-bound but not GDP-bound CDC42. Forms a tripartite complex with MYO18A and LURAP1 with the latter acting as an adapter connecting CDC42BPA and MYO18A. LURAP1 binding results in activation of CDC42BPA by abolition of its negative autoregulation. Interacts with LURAP1. Interacts (via AGC-kinase C-terminal domain) with FAM89B/LRAP25 (via LRR repeat). Forms a tripartite complex with FAM89B/LRAP25 and LIMK1.

Subcellular location. Cytoplasm. Cell projection. Lamellipodium.

Tissue specificity. Abundant in the heart, brain, skeletal muscle, kidney, and pancreas, with little or no expression in the lung and liver.

Post-translational modifications. Proteolytically cleaved by caspases upon apoptosis induction. The cleavage at Asp-478 by CASP3 increases its kinase activity (in vitro).

Activity regulation. Maintained in an inactive, closed conformation by an interaction between the kinase domain and the negative autoregulatory C-terminal coiled-coil region. Agonist binding to the phorbol ester binding site disrupts this, releasing the kinase domain to allow N-terminus-mediated dimerization and kinase activation by transautophosphorylation. Inhibited by chelerythrine chloride.

Induction. Regulated by cellular iron levels.

Similarity. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. DMPK subfamily.

Isoforms (6)

UniProt ID	Names	Canonical?
Q5VT25-1	1	yes
Q5VT25-2	2
Q5VT25-3	3
Q5VT25-4	4
Q5VT25-5	5
Q5VT25-6	6

RefSeq proteins (7): NP_001352939, NP_001352940, NP_001352948, NP_001374479, NP_001380943, NP_003598, NP_055641 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000095	CRIB_dom	Domain
IPR000719	Prot_kinase_dom	Domain
IPR000961	AGC-kinase_C	Domain
IPR001180	CNH_dom	Domain
IPR001849	PH_domain	Domain
IPR002219	PKC_DAG/PE	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR011993	PH-like_dom_sf	Homologous_superfamily
IPR014930	Myotonic_dystrophy_kinase_coil	Domain
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR017892	Pkinase_C	Domain
IPR026611	MRCK_alpha_cat	Domain
IPR031597	KELK	Domain
IPR046349	C1-like_sf	Homologous_superfamily
IPR050839	Rho-assoc_Ser/Thr_Kinase	Family
IPR057529	MRCK/ROCK_PH	Domain

Pfam: PF00069, PF00130, PF00433, PF00780, PF08826, PF15796, PF25346

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (66 total): modified residue 14, sequence variant 13, mutagenesis site 9, splice variant 6, domain 5, compositionally biased region 4, sequence conflict 4, coiled-coil region 2, binding site 2, site 2, region of interest 2, chain 1, active site 1, zinc finger region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q5VT25-F1	75.69	0.30

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 (3): 201 (proton acceptor); 478–479 (cleavage; by casp3 in vitro); 984–985 (cleavage; by casp3 in vitro)

Ligand- & substrate-binding residues (2): 83–91; 106

Post-translational modifications (14): 222, 234, 240, 1127, 1545, 1611, 1613, 1629, 1651, 1664, 1669, 1693, 1719, 1721

Mutagenesis-validated functional residues (9):

Position	Phenotype
106	loss of kinase activity.
222	increase in autophosphorylation but not kinase activity.
234	loss of autophosphorylation and kinase activity.
240	loss of autophosphorylation and kinase activity.
403	loss of autophosphorylation and kinase activity.
478	prevents cleavage by casp3, impairs the increase of its kinase activity and impairs extrusion apical actin ring assembly
984	prevents cleavage by casp3.
1579	loss of cdc42 binding; when associated with a-1582.
1582	loss of cdc42 binding; when associated with a-1579.

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-9013148	CDC42 GTPase cycle
R-HSA-9013149	RAC1 GTPase cycle
R-HSA-9013406	RHOQ GTPase cycle
R-HSA-9013409	RHOJ GTPase cycle
R-HSA-162582	Signal Transduction
R-HSA-194315	Signaling by Rho GTPases
R-HSA-9012999	RHO GTPase cycle
R-HSA-9716542	Signaling by Rho GTPases, Miro GTPases and RHOBTB3

MSigDB gene sets: 218 (showing top): BORCZUK_MALIGNANT_MESOTHELIOMA_UP, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, MITSIADES_RESPONSE_TO_APLIDIN_DN, TGACCTY_ERR1_Q2, MORF_RAD51L3, MARTINEZ_RB1_TARGETS_UP, ONKEN_UVEAL_MELANOMA_UP, SHEDDEN_LUNG_CANCER_GOOD_SURVIVAL_A4, DACOSTA_UV_RESPONSE_VIA_ERCC3_TTD_DN, MORF_PRKCA, GOBP_ACTOMYOSIN_STRUCTURE_ORGANIZATION, DACOSTA_UV_RESPONSE_VIA_ERCC3_COMMON_DN, PYEON_CANCER_HEAD_AND_NECK_VS_CERVICAL_UP, SAKAI_TUMOR_INFILTRATING_MONOCYTES_UP, VANTVEER_BREAST_CANCER_POOR_PROGNOSIS

GO Biological Process (5): protein phosphorylation (GO:0006468), cell migration (GO:0016477), actin cytoskeleton organization (GO:0030036), actomyosin structure organization (GO:0031032), cytoskeleton organization (GO:0007010)

GO Molecular Function (12): magnesium ion binding (GO:0000287), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), zinc ion binding (GO:0008270), identical protein binding (GO:0042802), protein serine kinase activity (GO:0106310), 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 (10): cytoplasm (GO:0005737), cytosol (GO:0005829), cytoskeleton (GO:0005856), cell-cell junction (GO:0005911), lamellipodium (GO:0030027), cell leading edge (GO:0031252), actomyosin (GO:0042641), extracellular exosome (GO:0070062), membrane (GO:0016020), cell projection (GO:0042995)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
RHO GTPase cycle	4
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1
Signaling by Rho GTPases	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	6
protein kinase activity	2
phosphorylation	1
protein modification process	1
cell motility	1
cytoskeleton organization	1
actin filament-based process	1
actin cytoskeleton organization	1
organelle organization	1
metal ion binding	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transition metal ion binding	1
protein 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
intracellular anatomical structure	1
cytoplasm	1
intracellular membraneless organelle	1
anchoring junction	1
cell leading edge	1
plasma membrane bounded cell projection	1
actin cytoskeleton	1
extracellular vesicle	1

Protein interactions and networks

STRING

2594 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CDC42BPA	CDC42	P21181	994
CDC42BPA	LURAP1	Q96LR2	988
CDC42BPA	MYL9	P24844	758
CDC42BPA	RHOA	P06749	708
CDC42BPA	PPP1R12C	Q9BZL4	700
CDC42BPA	MYO18A	Q92614	642
CDC42BPA	PPP1R12A	O14974	552
CDC42BPA	LIMK2	P53671	515
CDC42BPA	MYL12B	O14950	494
CDC42BPA	CFL2	Q9Y281	490
CDC42BPA	CFL1	P23528	490
CDC42BPA	CDC14A	Q9UNH5	487
CDC42BPA	WASL	O00401	448
CDC42BPA	PPP1CB	P37140	440
CDC42BPA	MYL2	P10916	434

IntAct

113 interactions, top by confidence:

A	B	Type	Score
CDKN2D	CDK4	psi-mi:“MI:0914”(association)	0.970
CDC42	CDC42BPA	psi-mi:“MI:0915”(physical association)	0.820
CDC42BPA	CDC42	psi-mi:“MI:0407”(direct interaction)	0.820
CDC42BPA	CDC42	psi-mi:“MI:0403”(colocalization)	0.820
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CDC42BPA	CDC42BPA	psi-mi:“MI:0407”(direct interaction)	0.710
CDC42BPA	CDC42BPA	psi-mi:“MI:0217”(phosphorylation reaction)	0.710
YWHAG	BLTP3B	psi-mi:“MI:2364”(proximity)	0.640
CSNK2B	RPS6KA4	psi-mi:“MI:0914”(association)	0.640
YWHAH	PLEKHG3	psi-mi:“MI:0914”(association)	0.610
YWHAH	BLTP3B	psi-mi:“MI:2364”(proximity)	0.570
YWHAZ	BLTP3B	psi-mi:“MI:0914”(association)	0.530
SLC31A1	C2orf72	psi-mi:“MI:0914”(association)	0.530
HAVCR2	TCAF2	psi-mi:“MI:0914”(association)	0.530
KCTD17	CBX4	psi-mi:“MI:0914”(association)	0.530
PTGES3	AIP	psi-mi:“MI:0914”(association)	0.530
LURAP1	TRIM24	psi-mi:“MI:0914”(association)	0.530
SRSF5	CBX6	psi-mi:“MI:0914”(association)	0.530

BioGRID (201): CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS), CDC42BPA (Affinity Capture-MS)

ESM2 similar proteins: A0JMA8, A1A5P5, A5WW21, E7F187, E7FDW2, O01583, O14827, O35711, O43150, O54874, P28818, P33175, Q08CX1, Q12756, Q12840, Q21653, Q22908, Q2KI89, Q3UP38, Q3UU96, Q5R629, Q5R9K7, Q5RI75, Q5U245, Q5VT25, Q5W7F2, Q619T5, Q6NRC9, Q6QLM7, Q7SIG6, Q7TT49, Q7TT50, Q7Z3E5, Q86W92, Q8C8U0, Q8CIS0, Q8IZ41, Q8LNZ2, Q8ND30, Q8R0Z2

Diamond homologs: A0A7J6K7I9, A0A7J6K7Y0, A0A7J6KD88, A8X775, B1WAR9, C4YRB7, D2HXI8, E1C2I2, E9PSL7, G1X456, G5EGQ3, M3TYT0, O00506, O01583, O01700, O14578, O54874, O61267, O75116, O77819, O80902, O88643, O97627, P05131, P0CY23, P0CY24, P13677, P21146, P25098, P26817, P26818, P32865, P34100, P35465, P38070, P48562, P49025, P49673, P54265, P70335

SIGNOR signaling

10 interactions.

A	Effect	B	Mechanism
CDC42BPA	up-regulates	MYL9	phosphorylation
CDC42	“up-regulates activity”	CDC42BPA	binding
CDC42BPA	“up-regulates activity”	LIMK2	phosphorylation
CDC42BPA	“up-regulates activity”	LIMK1	phosphorylation
CDC42BPA	“up-regulates activity”	MYL2	phosphorylation
CDC42BPA	“down-regulates activity”	PPP1R12C	phosphorylation
CDC42BPA	“up-regulates activity”	CDC42BPA	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 110 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
SARS-CoV-1 targets host intracellular signalling and regulatory pathways	8	71.7×	3e-11
Activation of BAD and translocation to mitochondria	7	71.1×	4e-10
Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex	7	62.7×	1e-09
Activation of BH3-only proteins	7	46.3×	7e-09
RHO GTPases activate PKNs	8	33.8×	6e-09
Intrinsic Pathway for Apoptosis	7	27.3×	3e-07
Signaling by FGFR1 in disease	6	23.4×	7e-06
FOXO-mediated transcription	5	22.4×	5e-05

GO biological processes:

GO term	Partners	Fold	FDR
protein targeting	5	18.7×	2e-03
intracellular protein localization	9	9.6×	3e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	174
Likely benign	8
Benign	6

Top pathogenic / likely-pathogenic (0)

SpliceAI

7484 predictions. Top by Δscore:

Variant	Effect	Δscore
1:227004993:CTTG:C	donor_gain	1.0000
1:227016063:CT:C	donor_gain	1.0000
1:227016068:AATT:A	donor_gain	1.0000
1:227016075:CTTA:C	donor_loss	1.0000
1:227016077:T:TG	donor_loss	1.0000
1:227016908:C:CT	donor_gain	1.0000
1:227016909:T:TT	donor_gain	1.0000
1:227016928:T:TA	donor_gain	1.0000
1:227016945:T:A	donor_gain	1.0000
1:227017046:CCCTT:C	acceptor_gain	1.0000
1:227017047:CCTTC:C	acceptor_gain	1.0000
1:227017048:CTT:C	acceptor_gain	1.0000
1:227017051:C:CC	acceptor_gain	1.0000
1:227026050:ATTAC:A	donor_loss	1.0000
1:227026051:TTACC:T	donor_loss	1.0000
1:227026052:TACCT:T	donor_loss	1.0000
1:227026053:A:C	donor_loss	1.0000
1:227028656:CAA:C	donor_gain	1.0000
1:227029246:AATTT:A	acceptor_gain	1.0000
1:227029247:ATTT:A	acceptor_gain	1.0000
1:227029248:TTT:T	acceptor_gain	1.0000
1:227029249:TT:T	acceptor_gain	1.0000
1:227029250:TCTAA:T	acceptor_loss	1.0000
1:227029251:C:A	acceptor_loss	1.0000
1:227029251:C:CC	acceptor_gain	1.0000
1:227030407:CCAT:C	donor_gain	1.0000
1:227030470:TC:T	acceptor_loss	1.0000
1:227030471:C:CC	acceptor_gain	1.0000
1:227030473:A:AC	acceptor_gain	1.0000
1:227030473:A:C	acceptor_gain	1.0000

AlphaMissense

11616 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:227016127:G:C	H1582D	1.000
1:227016134:G:C	H1579Q	1.000
1:227016134:G:T	H1579Q	1.000
1:227016135:T:C	H1579R	1.000
1:227016136:G:C	H1579D	1.000
1:227016140:A:C	F1577L	1.000
1:227016140:A:T	F1577L	1.000
1:227016141:A:C	F1577C	1.000
1:227016141:A:G	F1577S	1.000
1:227016142:A:G	F1577L	1.000
1:227016159:A:T	I1571N	1.000
1:227026081:A:G	W1480R	1.000
1:227026081:A:T	W1480R	1.000
1:227026134:A:G	L1462P	1.000
1:227028681:A:G	W1448R	1.000
1:227028681:A:T	W1448R	1.000
1:227028732:C:A	G1431W	1.000
1:227028752:A:G	L1424P	1.000
1:227031433:A:G	W1192R	1.000
1:227031433:A:T	W1192R	1.000
1:227033341:A:T	I1162K	1.000
1:227033374:A:T	V1151D	1.000
1:227033389:A:T	V1146D	1.000
1:227034762:C:A	W1101C	1.000
1:227034762:C:G	W1101C	1.000
1:227034764:A:G	W1101R	1.000
1:227034764:A:T	W1101R	1.000
1:227040188:A:G	C1026R	1.000
1:227073960:A:G	L880P	1.000
1:227074332:A:G	L838P	1.000

dbSNP variants (sampled 300 via entrez): RS1000001399 (1:227162026 T>C), RS1000007031 (1:227167568 C>T), RS1000009738 (1:227296187 G>A,C), RS1000013904 (1:226996345 T>C), RS1000022176 (1:227288339 T>C), RS1000057807 (1:227300845 G>C), RS1000058128 (1:227217075 A>G), RS1000064025 (1:227173082 T>C), RS1000067521 (1:227080942 T>C), RS1000071968 (1:227208546 A>C), RS1000082457 (1:227044640 G>C,T), RS1000094240 (1:227002456 A>C,G), RS1000103765 (1:227166603 C>A), RS1000117370 (1:227232209 G>A), RS1000118903 (1:227161766 C>A,T)

Disease associations

OMIM: gene MIM:603412 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

24 associations (top):

Study	Trait	p-value
GCST002764_1	Optic cup area	2.000000e-07
GCST002765_2	Optic disc area	4.000000e-14
GCST002765_7	Optic disc area	2.000000e-12
GCST002927_17	Mercury levels	2.000000e-06
GCST004076_1	Optic disc area	1.000000e-14
GCST004076_17	Optic disc area	4.000000e-16
GCST004280_93	Diastolic blood pressure	8.000000e-09
GCST004626_9	Myeloid white cell count	4.000000e-11
GCST006976_105	Macular thickness	2.000000e-12
GCST006988_78	Blond vs. brown/black hair color	1.000000e-08
GCST008062_121	Blood urea nitrogen levels	3.000000e-08
GCST009404_20	Optic cup area	8.000000e-11
GCST009411_1	Optic disc area	7.000000e-17
GCST009462_52	Optic disc size	6.000000e-48
GCST009724_89	Vertical cup-disc ratio (multi-trait analysis)	3.000000e-16
GCST010482_5	Cardiovascular death or myocardial infarction in response to clopidogrel treatment	2.000000e-06
GCST011347_7	Low density lipoprotein cholesterol levels	6.000000e-09
GCST011703_41	Smoking initiation	6.000000e-09
GCST012256_20	SAPHO syndrome	3.000000e-07
GCST90002398_512	Neutrophil count	3.000000e-24
GCST90002407_204	White blood cell count	3.000000e-18
GCST90020029_600	Waist circumference adjusted for body mass index	5.000000e-08
GCST90020029_601	Waist circumference adjusted for body mass index	2.000000e-08
GCST90020029_602	Waist circumference adjusted for body mass index	8.000000e-11

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0006336	diastolic blood pressure
EFO:0003924	hair color
EFO:0006939	cup-to-disc ratio measurement
EFO:0006919	cardiovascular event measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0005670	smoking initiation
EFO:0004833	neutrophil count
EFO:0007789	BMI-adjusted waist circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4516 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

13 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 80,837 (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
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL5416410	DASATINIB	4	655
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL603469	LESTAURTINIB	3
CHEMBL103667	DORAMAPIMOD	2	1,681
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL1667969	SAR-407899 FREE BASE	2	157
CHEMBL1967878	CENISERTIB	2	358
CHEMBL1980715	LAUROGUADINE	2	294
CHEMBL3039513	DECERNOTINIB	2	1,418
CHEMBL574737	UCN-01	2	2,217
CHEMBL1084546	PF-00562271	1	399
CHEMBL3545083	RGB-286638	1	551

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — GEK subfamily

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
RKI-1447	Inhibition	8.54	pIC50
compound 11d [DOI: 10.1039/c0md00194e]	Inhibition	7.13	pIC50

Binding affinities (BindingDB)

65 measured of 66 human assays (66 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
8-(3-pyrimidin-4-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1,8-diazaspiro[5.5]undecane	KI	0.014 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(6S)-1-methyl-8-(3-pyrimidin-4-yl-1H-pyrrolo[2,3- b]pyridin-4-yl)-1,8-diazaspiro[5.5]undecane	KI	0.019 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(6S)-1-ethyl-8-(3-pyrimidin-4-yl-1H-pyrrolo[2,3- b]pyridin-4-yl)-1,8-diazaspiro[5.5]undecane	KI	0.028 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(6S)-8-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)- 1,8-diazaspiro[5.5]undecane	KI	0.028 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(5S)-2-(3-pyrimidin-4-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)- 2,6-diazaspiro[4.5]decane	KI	0.032 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(5S)-2-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)- 2,6-diazaspiro[4.5]decane	KI	0.041 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(6S)-8-[3-(2-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1,8- diazaspiro[5.5]undecane	KI	0.043 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-[3-(5-fluoro-3-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]- 1,8-diazaspiro[5.5]undecane	KI	0.064 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-(3-pyrazin-2-yl-1H- pyrrolo[2,3-b]pyridin-4-yl)- 1,8- diazaspiro[5.5]undecane	KI	0.131 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-[3-(5-fluoro-2-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]- 1,8-diazaspiro[5.5]undecane	KI	0.17 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-[3-(3-fluoro-2-pyridyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]- 1,8-diazaspiro[5.5]undecane	KI	0.189 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
N-[[(3R)-3-aminopiperidin-3-yl]methyl]-3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-amine	KI	0.189 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-methyl-1-(3-pyrimidin-4-yl-1H-pyrrolo[2,3- b]pyridin-4-yl)piperidin-3-amine	KI	0.238 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-[(6S)-1,8-diazaspiro[5.5]undecan-8-yl]-1H- pyrrolo[2,3-b]pyridine-3-carbonitrile	KI	0.249 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-(3-pyridazin-3-yl-1H- pyrrolo[2,3-b]pyridin-4-yl)- 1,8- diazaspiro[5.5]undecane	KI	0.257 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-methyl-1-(3- pyridazin-4-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	0.274 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-cyclopropyl-1-(3-pyridazin-4-yl-1H-pyrrolo[2,3- b]pyridin-4-yl)piperidin-3-amine	KI	0.322 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea	KD	0.37 nM
N-methyl-1-(3-pyrimidin- 5-yl-1H-pyrrolo[2,3- b]pyridin-4-yl)azepan-4- amine	KI	0.382 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-(2,6-diazaspiro[4.5]decan-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile	KI	0.481 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
3-methyl-1-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	0.517 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-methyl-1-(3- pyridazin-3-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	0.566 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-[3-(1-methylpyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1,8-diazaspiro[5.5]undecane	KI	0.598 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-methyl-1-(3- pyrazin-2-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	0.629 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-(1-ethyl-1,8-diazaspiro[5.5]undecan-8-yl)-1H- pyrrolo[2,3-b]pyridine-3-carbonitrile	KI	0.631 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
2-(3-pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridin-4-yl)- 2,8- diazaspiro[5.5]undecane	KI	0.652 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-cyclopropyl-1-(3- pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	0.935 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-(azepan-4-yloxy)-3- pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridine	KI	1.13 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-ethyl-1-(3- pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	1.23 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
8-(3-pyrimidin-2-yl-1H- pyrrolo[2,3-b]pyridin-4-yl)- 1,8- diazaspiro[5.5]undecane	KI	1.34 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
Staurosporine	KD	1.7 nM
4-[(6R)-1,8- diazaspiro[5.5]undecan-8- yl]-1H-pyrrolo[2,3- b]pyridine-3-carbonitrile	KI	1.83 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-1-methyl-3-[(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxymethyl]piperidin-3-amine	KI	1.91 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
3-pyrimidin-5-yl-4- [[(3R)-pyrrolidin-3- yl]methoxy]-1H- pyrrolo[2,3-b]pyridine	KI	2.52 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(6R)-8-(3-pyrimidin-4-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)-1,8-diazaspiro[5.5]undecane	KI	2.89 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-N-methyl-1-(3- pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridin-4- yl)piperidin-3-amine	KI	2.93 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
Phorbol ester (PDBU)	KD	3.4 nM
(3S)-N-ethyl-1-[3-(1- methylpyrazol-4-yl)-1H- pyrrolo[2,3-b]pyridin-4- yl]piperidin-3-amine	KI	3.48 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
(3S)-1-(3-pyrimidin-5-yl- 1H-pyrrolo[2,3-b]pyridin- 4-yl)piperidin-3-amine	KI	4.5 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-[(2R)-2-methylpyrrolidin- 1-yl]-1H-pyrrolo[2,3- b]pyridine-3-carbonitrile	KI	4.6 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
[1-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-yl]methanamine	KI	4.6 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
9-(3-pyrimidin-5-yl-1H- pyrrolo[2,3-b]pyridin-4-yl)- 1,9-diazaspiro[4.5]decane	KI	4.69 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-[(3S)-3-(azetidin-1-yl)- 1-piperidyl]-3-pyrimidin- 5-yl-1H-pyrrolo[2,3- b]pyridine	KI	5.2 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
3-pyrimidin-5-yl-4-[(3S)- 3-pyrrolidin-1-yl-1- piperidyl]-1H-pyrrolo[2,3- b]pyridine	KI	5.8 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-[(3S)-3-(1-piperidyl)-1- piperidyl]-3-pyrimidin-5- yl-1H-pyrrolo[2,3- b]pyridine	KI	7.9 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
1-[1-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-yl]pyrrolidin-3-amine	KI	11.6 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
4-[4-(4-fluorophenyl)-2-(4-methanesulfinylphenyl)-1H-imidazol-5-yl]pyridine	KD	12 nM
(3S)-N,N-dimethyl-1-(3-pyrimidin-5-yl-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-amine	KI	17.2 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
Sapintoxin D	KI	18.2 nM
(3S)-N-methyl-1-[3-(1- methylpyrazol-4-yl)-1H- pyrrolo[2,3-b]pyridin-4- yl]piperidin-3-amine	KI	18.9 nM	US-11447505: Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer

ChEMBL bioactivities

365 potent at pChembl≥5 of 367 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.92	Ki	0.012	nM	CHEMBL5811574
10.85	Ki	0.014	nM	CHEMBL5764454
10.82	Ki	0.015	nM	CHEMBL6014969
10.72	Ki	0.019	nM	CHEMBL5963387
10.68	Ki	0.021	nM	CHEMBL5742314
10.55	Ki	0.028	nM	CHEMBL5946285
10.55	Ki	0.028	nM	CHEMBL5871406
10.49	Ki	0.032	nM	CHEMBL5927623
10.48	Ki	0.033	nM	CHEMBL5834378
10.39	Ki	0.041	nM	CHEMBL5861512
10.37	Ki	0.043	nM	CHEMBL5762036
10.31	Ki	0.049	nM	CHEMBL5816740
10.28	Ki	0.052	nM	CHEMBL5968389
10.19	Ki	0.064	nM	CHEMBL5863351
10.17	Ki	0.068	nM	CHEMBL5796818
10.09	Ki	0.082	nM	CHEMBL5976859
10.03	Ki	0.093	nM	CHEMBL5826180
10.02	Ki	0.095	nM	CHEMBL5811574
10.00	Ki	0.101	nM	CHEMBL5783588
9.90	Ki	0.127	nM	CHEMBL5958092
9.88	Ki	0.131	nM	CHEMBL5827582
9.80	Ki	0.158	nM	CHEMBL5741390
9.77	Ki	0.17	nM	CHEMBL5808035
9.73	Ki	0.185	nM	CHEMBL5807019
9.72	Ki	0.189	nM	CHEMBL6027343
9.72	Ki	0.19	nM	CHEMBL6021899
9.72	Ki	0.189	nM	CHEMBL5832781
9.68	Ki	0.207	nM	CHEMBL6042256
9.67	Ki	0.216	nM	CHEMBL5952618
9.66	Ki	0.217	nM	CHEMBL6045435
9.62	Ki	0.238	nM	CHEMBL5859006
9.60	Ki	0.249	nM	CHEMBL6060859
9.59	Ki	0.257	nM	CHEMBL5856790
9.56	Ki	0.274	nM	CHEMBL6034159
9.49	Ki	0.322	nM	CHEMBL6031197
9.42	Ki	0.382	nM	CHEMBL5995288
9.32	Ki	0.481	nM	CHEMBL5912414
9.32	Ki	0.481	nM	CHEMBL5871280
9.29	Ki	0.517	nM	CHEMBL5775722
9.28	Ki	0.522	nM	CHEMBL5953716
9.25	Ki	0.566	nM	CHEMBL5792987
9.22	Ki	0.598	nM	CHEMBL5877531
9.20	Ki	0.631	nM	CHEMBL5889627
9.20	Ki	0.629	nM	CHEMBL5994105
9.19	Ki	0.652	nM	CHEMBL5978419
9.03	Ki	0.935	nM	CHEMBL5808093
9.00	IC50	0.998	nM	STAUROSPORINE
8.96	Ki	1.11	nM	CHEMBL6004633
8.95	Ki	1.13	nM	CHEMBL5941238
8.91	Ki	1.23	nM	CHEMBL5843535

PubChem BioAssay actives

62 with measured affinity, of 929 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
(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	1715261: Inhibition of human MRCKalpha using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate by [gamma-33P]-ATP assay	ic50	0.0010	uM
1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea;methanesulfonic acid	1119790: Inhibition of MRCKalpha (unknown origin)	ic50	0.0029	uM
[(1R,6R,13R,14R,15S)-13-butanoyloxy-1,6-dihydroxy-4,12,12,15-tetramethyl-5,8-dioxo-14-tetracyclo[8.5.0.02,6.011,13]pentadec-3-enyl] 2-(methylamino)benzoate	1799804: Binding Assay from Article 10.1074/jbc.M707463200: “Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.”	ki	0.0059	uM
6-piperidin-4-yloxy-2H-isoquinolin-1-one	1424933: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0100	uM
[(1R,6R,13R,14R,15S)-13-butanoyloxy-1,6-dihydroxy-4,12,12,15-tetramethyl-5,8-dioxo-14-tetracyclo[8.5.0.02,6.011,13]pentadec-3-enyl] butanoate	1799804: Binding Assay from Article 10.1074/jbc.M707463200: “Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.”	kd	0.0103	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526300: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged CDC42BPA (unknown origin) (1 to 574 residues) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0250	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148036: Binding affinity to human CDC42BPA incubated for 45 mins by Kinobead based pull down assay	kd	0.0279	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526300: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged CDC42BPA (unknown origin) (1 to 574 residues) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0430	uM
N-[(1R,2S)-2-aminocyclohexyl]-4-[6-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]thiophene-2-carboxamide	1637059: Inhibition of recombinant human His-tagged CDC42BPA catalytic domain expressed in baculovirus expression system by Z’-LYTE assay	ic50	0.0720	uM
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-fluoro-3,4-dihydro-2H-chromene-3-carboxamide	371549: Inhibition of MRCKalpha	ic50	0.0790	uM
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-methoxy-3,4-dihydro-2H-chromene-3-carboxamide	371549: Inhibition of MRCKalpha	ic50	0.1500	uM
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-2H-chromene-3-carboxamide	371549: Inhibition of MRCKalpha	ic50	0.2100	uM
N-[2-(dimethylamino)ethyl]-N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1,3-benzothiazole-2-carboxamide	468087: Inhibition of MRCKalpha	ic50	0.2470	uM
(2S,3R,4R,6R,18S)-18-hydroxy-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	1424933: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2540	uM
(3R)-N-[2-[2-(dimethylamino)ethoxy]-5-fluoro-4-(1H-pyrazol-4-yl)phenyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide	499518: Inhibition of MRCKalpha	ic50	0.3330	uM
N-[2-methoxy-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide	1798560: MRCK Inhibition Assay from Article 10.1021/jm800986w: “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.”	ic50	0.3670	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	624920: Binding constant for MRCKA kinase domain	kd	0.3800	uM
(2R)-2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide	1424933: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.5610	uM
1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide	624920: Binding constant for MRCKA kinase domain	kd	0.6600	uM
(3R)-6-methoxy-N-[2-[(1-methylpiperidin-4-yl)methoxy]-4-(1H-pyrazol-4-yl)phenyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide	499518: Inhibition of MRCKalpha	ic50	0.6690	uM
(3R)-N-[2-[2-(dimethylamino)ethoxy]-5-fluoro-4-(1H-pyrazol-4-yl)phenyl]-2-ethyl-3,4-dihydro-1H-isoquinoline-3-carboxamide	499518: Inhibition of MRCKalpha	ic50	0.8100	uM
N-[(1R,6R)-6-amino-2,2-difluorocyclohexyl]-4-(6-chloropyrazolo[1,5-a]pyrimidin-3-yl)-5-methylthiophene-2-carboxamide	1637059: Inhibition of recombinant human His-tagged CDC42BPA catalytic domain expressed in baculovirus expression system by Z’-LYTE assay	ic50	1.0000	uM
[(4Z)-2-(hydroxymethyl)-4-[5-methyl-3-(2-methylpropyl)hexylidene]-5-oxooxolan-2-yl]methyl 2,2-dimethylpropanoate	1799804: Binding Assay from Article 10.1074/jbc.M707463200: “Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.”	ki	1.0330	uM
1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[2,1-d]pyrazol-5-yl]-3-morpholin-4-ylurea	1424933: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.0940	uM
N-[4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide	1798560: MRCK Inhibition Assay from Article 10.1021/jm800986w: “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.”	ic50	1.1900	uM
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide	1798560: MRCK Inhibition Assay from Article 10.1021/jm800986w: “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.”	ic50	1.1900	uM
4-[6-[4-(2-piperidin-1-ylethoxy)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-N-(2,2,2-trifluoroethyl)thiophene-2-carboxamide	1637059: Inhibition of recombinant human His-tagged CDC42BPA catalytic domain expressed in baculovirus expression system by Z’-LYTE assay	ic50	1.2000	uM
6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one	624920: Binding constant for MRCKA kinase domain	kd	1.3000	uM
1-ethyl-1-[(3-methoxyphenyl)methyl]-3-[2-[(3S)-1-methylpyrrolidin-3-yl]oxy-4-(1H-pyrazol-4-yl)phenyl]urea	735777: Inhibition of MRCKalpha (unknown origin) using LCD-AKRRRRLSSLRA-NH2 as substrate after 75 mins by luminescence assay in presence of [33P]ATP	ic50	1.5500	uM
3-(6-morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)phenol	436024: Binding constant for MRCKA kinase domain	kd	1.8000	uM
1-[(3-methoxyphenyl)methyl]-1-methyl-3-[4-(1H-pyrazol-4-yl)phenyl]urea	735777: Inhibition of MRCKalpha (unknown origin) using LCD-AKRRRRLSSLRA-NH2 as substrate after 75 mins by luminescence assay in presence of [33P]ATP	ic50	1.8530	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	436024: Binding constant for MRCKA kinase domain	kd	2.0000	uM
Vandetanib	436024: Binding constant for MRCKA kinase domain	kd	2.6000	uM
[(2S)-3-hydroxy-2-octanoyloxypropyl] octanoate	1799804: Binding Assay from Article 10.1074/jbc.M707463200: “Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.”	ki	2.8200	uM
1-(2-hydroxyethyl)-1-[(3-methoxyphenyl)methyl]-3-[4-(1H-pyrazol-4-yl)phenyl]urea	735777: Inhibition of MRCKalpha (unknown origin) using LCD-AKRRRRLSSLRA-NH2 as substrate after 75 mins by luminescence assay in presence of [33P]ATP	ic50	4.3060	uM
7-chloro-8-(3-hydroxypropyl)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5(10),6,8,18(22),19-hexaene-19-carbonitrile	281177: Inhibition of Cdc42BPA	ki	4.4400	uM
N-(4-pyridin-4-yl-1,3-thiazol-2-yl)-2,3-dihydro-1,4-benzodioxine-3-carboxamide	1798560: MRCK Inhibition Assay from Article 10.1021/jm800986w: “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.”	ic50	4.8500	uM
(3R)-N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide	499518: Inhibition of MRCKalpha	ic50	5.3500	uM
4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine	436024: Binding constant for MRCKA kinase domain	kd	6.2000	uM
1-[1-(3-fluorophenyl)-3-hydroxypropyl]-3-[4-(1H-pyrazol-4-yl)phenyl]urea	735777: Inhibition of MRCKalpha (unknown origin) using LCD-AKRRRRLSSLRA-NH2 as substrate after 75 mins by luminescence assay in presence of [33P]ATP	ic50	6.4000	uM
7-chloro-8-(3-hydroxypropoxy)-3-oxo-11,17-dioxa-2,4,20,22-tetrazatricyclo[16.3.1.05,10]docosa-1(21),5,7,9,18(22),19-hexaene-19-carbonitrile	281177: Inhibition of Cdc42BPA	ki	6.6300	uM
N-(4-pyridin-4-ylphenyl)-2,3-dihydro-1,4-benzodioxine-3-carboxamide	1798560: MRCK Inhibition Assay from Article 10.1021/jm800986w: “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.”	ic50	7.0500	uM
N-ethyl-N-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)-1,3-benzothiazole-2-carboxamide	468087: Inhibition of MRCKalpha	ic50	7.8610	uM
1-[2-(dimethylamino)ethyl]-1-[(3-methoxyphenyl)methyl]-3-[4-(1H-pyrazol-4-yl)phenyl]urea	735777: Inhibition of MRCKalpha (unknown origin) using LCD-AKRRRRLSSLRA-NH2 as substrate after 75 mins by luminescence assay in presence of [33P]ATP	ic50	8.6950	uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one	624920: Binding constant for MRCKA kinase domain	kd	9.2000	uM
4-[6-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]-N-(2,2,2-trifluoroethyl)thiophene-2-carboxamide	1637059: Inhibition of recombinant human His-tagged CDC42BPA catalytic domain expressed in baculovirus expression system by Z’-LYTE assay	ic50	9.2000	uM
1-[3-tert-butyl-1-(4-methylphenyl)pyrazol-5-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea	436024: Binding constant for MRCKA kinase domain	kd	9.4000	uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one	436024: Binding constant for MRCKA kinase domain	kd	9.5000	uM
N-[3-(dimethylamino)propyl]-3-[6-(1H-pyrazol-4-yl)-1,3-benzothiazol-2-yl]-3,4-dihydro-2H-chromene-6-carboxamide	468087: Inhibition of MRCKalpha	ic50	9.5520	uM
1-[4-(4-propanoylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-9-quinolin-3-ylbenzo[h][1,6]naphthyridin-2-one	517857: Binding affinity to MRCKA	kd	10.0000	uM

CTD chemical–gene interactions

54 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
arsenite	affects binding, decreases reaction, increases methylation	2
Arsenic Trioxide	increases expression	2
Valproic Acid	decreases expression	2
p-Chloromercuribenzoic Acid	affects cotreatment, increases expression	2
aristolochic acid I	decreases expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
bisphenol A	affects cotreatment, decreases methylation	1
terbufos	decreases methylation	1
sodium arsenite	increases expression	1
cobaltous chloride	decreases expression	1
butyraldehyde	decreases expression	1
potassium chromate(VI)	decreases expression	1
cupric chloride	increases expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
ICG 001	increases expression	1
abrine	decreases expression	1
dorsomorphin	affects cotreatment, increases expression	1
Irinotecan	decreases expression	1
Temozolomide	decreases expression	1
Sunitinib	increases expression	1
Fulvestrant	affects cotreatment, decreases methylation	1
Vorinostat	decreases expression	1
Arsenic	affects methylation	1
Atrazine	decreases expression	1
Azacitidine	decreases expression	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Caffeine	decreases phosphorylation	1
Carbamazepine	affects expression	1

ChEMBL screening assays

216 unique, capped per target: 215 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1048280	Binding	Inhibition of MRCKA assessed as enzyme activity at 1 uM relative to untreated control	Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. — J Med Chem
CHEMBL1964102	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CDC42BPA	PubChem BioAssay data set

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B1MW	Abcam HeLa CDC42BPA KO	Cancer cell line	Female
CVCL_XM65	HAP1 CDC42BPA (-) 1	Cancer cell line	Male
CVCL_XM66	HAP1 CDC42BPA (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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