CIT

Summary

CIT (citron rho-interacting serine/threonine kinase, HGNC:1985) is a protein-coding gene on chromosome 12q24.23, encoding Citron Rho-interacting kinase (O14578). Plays a role in cytokinesis. It is a selective cancer dependency (DepMap: 49.4% of cell lines).

This gene encodes a serine/threonine-protein kinase that functions in cell division. Together with the kinesin KIF14, this protein localizes to the central spindle and midbody, and functions to promote efficient cytokinesis. This protein is involved in central nervous system development. Polymorphisms in this gene are associated with bipolar disorder and risk for schizophrenia. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 11113 — RefSeq curated summary.

At a glance

• Gene–disease (curated): microcephaly 17, primary, autosomal recessive (Strong, GenCC) — +1 more curated relationship
• GWAS associations: 3
• Clinical variants (ClinVar): 777 total — 17 pathogenic, 8 likely-pathogenic
• Phenotypes (HPO): 40
• Druggable target: yes — 41 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 49.4% of screened cell lines
• MANE Select transcript: NM_001206999

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1985
Approved symbol	CIT
Name	citron rho-interacting serine/threonine kinase
Location	12q24.23
Locus type	gene with protein product
Status	Approved
Aliases	KIAA0949, STK21, CRIK, CITK
Ensembl gene	ENSG00000122966
Ensembl biotype	protein_coding
OMIM	605629
Entrez	11113

Gene structure

Transcript identifiers

Ensembl transcripts: 42 — 19 retained_intron, 14 protein_coding, 7 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined

ENST00000261833, ENST00000392520, ENST00000392521, ENST00000469414, ENST00000488203, ENST00000536008, ENST00000536325, ENST00000537607, ENST00000538073, ENST00000543239, ENST00000543324, ENST00000544588, ENST00000544800, ENST00000544872, ENST00000545913, ENST00000546026, ENST00000676563, ENST00000676693, ENST00000676833, ENST00000676849, ENST00000677438, ENST00000677738, ENST00000677742, ENST00000677812, ENST00000677849, ENST00000677927, ENST00000677993, ENST00000678087, ENST00000678155, ENST00000678236, ENST00000678494, ENST00000678652, ENST00000678677, ENST00000678686, ENST00000678708, ENST00000679061, ENST00000679120, ENST00000679249, ENST00000679285, ENST00000867920, ENST00000928243, ENST00000928244

RefSeq mRNA: 2 — MANE Select: NM_001206999 NM_001206999, NM_007174

CCDS: CCDS55891, CCDS9192

Canonical transcript exons

ENST00000392521 — 48 exons

Exon	Start	End
ENSE00000835227	119718699	119718861
ENSE00001034406	119834086	119834228
ENSE00001034408	119857523	119857698
ENSE00001034409	119825165	119825368
ENSE00001034410	119822820	119822973
ENSE00001034411	119850174	119850275
ENSE00001034414	119832771	119832864
ENSE00001034415	119869060	119869201
ENSE00001131908	119876073	119876181
ENSE00002205195	119685791	119688255
ENSE00002320098	119877249	119877320
ENSE00003462941	119720478	119720585
ENSE00003473907	119713468	119713648
ENSE00003474856	119775786	119775839
ENSE00003475110	119776672	119776842
ENSE00003476651	119701624	119701752
ENSE00003499242	119714197	119714334
ENSE00003500492	119803206	119803389
ENSE00003500862	119710540	119710620
ENSE00003502716	119757371	119757545
ENSE00003506319	119728502	119728606
ENSE00003513108	119776358	119776408
ENSE00003514604	119742411	119742464
ENSE00003515254	119701850	119701958
ENSE00003516482	119772770	119772910
ENSE00003517456	119758591	119758700
ENSE00003528745	119690151	119690454
ENSE00003546957	119712591	119712695
ENSE00003549731	119783908	119784051
ENSE00003550662	119770785	119770910
ENSE00003553412	119734164	119734357
ENSE00003553792	119782518	119782637
ENSE00003582260	119700745	119700825
ENSE00003589687	119704363	119704455
ENSE00003601874	119718245	119718409
ENSE00003612090	119784960	119785065
ENSE00003624689	119735160	119735357
ENSE00003625070	119708179	119708318
ENSE00003626669	119760939	119761055
ENSE00003636301	119697659	119697838
ENSE00003639544	119697976	119698054
ENSE00003643151	119712178	119712347
ENSE00003644069	119767087	119767182
ENSE00003651773	119721309	119721449
ENSE00003658288	119752050	119752247
ENSE00003672853	119713203	119713294
ENSE00003686023	119710251	119710386
ENSE00003785330	119730495	119730630

Expression profiles

Bgee: expression breadth ubiquitous, 232 present calls, max score 96.50.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 10.5709 / max 344.4867, expressed in 1349 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter ID	TPM avg	Samples expressed
133586	3.8531	1072
133581	2.6083	176
133585	2.4693	892
133584	0.9774	126
133582	0.3141	108
133583	0.1427	60
133577	0.0502	13
133575	0.0489	10
133573	0.0390	19
133568	0.0348	6

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lateral nuclear group of thalamus	UBERON:0002736	96.50	gold quality
right frontal lobe	UBERON:0002810	96.16	gold quality
sural nerve	UBERON:0015488	95.67	gold quality
primary visual cortex	UBERON:0002436	95.04	gold quality
Brodmann (1909) area 9	UBERON:0013540	94.99	gold quality
caudate nucleus	UBERON:0001873	94.55	gold quality
putamen	UBERON:0001874	94.54	gold quality
postcentral gyrus	UBERON:0002581	94.41	gold quality
cingulate cortex	UBERON:0003027	94.26	gold quality
anterior cingulate cortex	UBERON:0009835	94.24	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	94.07	gold quality
nucleus accumbens	UBERON:0001882	93.86	gold quality
parietal lobe	UBERON:0001872	93.71	gold quality
occipital lobe	UBERON:0002021	93.62	gold quality
Brodmann (1909) area 10	UBERON:0013541	93.41	gold quality
superior frontal gyrus	UBERON:0002661	93.13	gold quality
frontal cortex	UBERON:0001870	93.08	gold quality
neocortex	UBERON:0001950	92.88	gold quality
frontal pole	UBERON:0002795	92.79	gold quality
telencephalon	UBERON:0001893	92.34	gold quality
prefrontal cortex	UBERON:0000451	92.31	gold quality
cerebral cortex	UBERON:0000956	92.00	gold quality
amygdala	UBERON:0001876	91.76	gold quality
forebrain	UBERON:0001890	91.25	gold quality
middle frontal gyrus	UBERON:0002702	91.24	gold quality
Brodmann (1909) area 46	UBERON:0006483	91.23	gold quality
middle temporal gyrus	UBERON:0002771	90.90	gold quality
temporal lobe	UBERON:0001871	90.69	gold quality
right hemisphere of cerebellum	UBERON:0014890	90.65	gold quality
hypothalamus	UBERON:0001898	90.58	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-HCAD-35	yes	446.37
E-MTAB-6678	yes	133.19
E-ANND-3	yes	18.77
E-MTAB-9543	no	2.42

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

118 targeting CIT, 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-4481	100.00	66.42	1669
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-4745-5P	99.98	65.95	1028
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-4725-3P	99.96	69.53	2520
HSA-MIR-6780B-5P	99.96	69.60	2562
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-338-5P	99.92	72.34	2951
HSA-MIR-454-3P	99.91	74.01	1925
HSA-MIR-130B-3P	99.90	73.27	1850
HSA-MIR-3666	99.90	73.24	1833
HSA-MIR-130A-3P	99.90	73.31	1861
HSA-MIR-301A-3P	99.90	73.15	1839
HSA-MIR-301B-3P	99.90	73.19	1836
HSA-MIR-4295	99.90	73.11	1838
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-95-5P	99.89	72.17	3973
HSA-MIR-4271	99.88	68.32	2244
HSA-MIR-30A-3P	99.87	69.74	2928
HSA-MIR-30D-3P	99.87	69.92	2917
HSA-MIR-30E-3P	99.87	69.68	2942
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-3714	99.71	70.74	2671

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 49.4% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 27)

• Citron-K has a distinct cell cycle-dependent expression pattern and cellular localization as a downstream target of Rho-GTPase and functions in the control of G(2)/M transition in the hepatocyte cell cycle (PMID:12411428)
• Single nucleotide polymorphisms associated with bipolar disorder. (PMID:15983625)
• During cytokinesis, the localization of KIF14 and citron kinase to the central spindle and midbody is codependent, and they form a complex depending on the activation state of citron kinase. (PMID:16431929)
• ASPM and citron kinase co-localize to the midbody ring during cytokinesis. (PMID:17534152)
• Evidence of statistical epistasis between DISC1, CIT and NDEL1 impacting risk for schizophrenia: biological validation with functional neuroimaging. (PMID:20084519)
• CITRON has a role in proliferation of hepatocellular carcinoma cells (PMID:20369383)
• Hrs inhibits HIV-1 production by inhibiting citron kinase-mediated exocytosis. (PMID:21748597)
• CIT-K is a crucial abscission regulator that may promote midbody stability through active RhoA and anillin. (PMID:21849473)
• p27 has a role in cytokinesis via the regulation of citron-K activity (PMID:22293177)
• High CIT expression is associated with prostate cancer. (PMID:22761715)
• Data propose that the CC-domain-mediated translocation and actions of Citron-K ensure proper stabilization of the midbody structure during the transition from constriction to abscission. (PMID:23444367)
• The TPC1 was shown to interact with citron kinase, with TPC1 overexpression affecting RhoA activity and myosin light chain phosphorylation levels in cytokinesis. (PMID:25665131)
• HIV-1 infection upregulates citK expression at the transcriptional level (PMID:26524911)
• The CIT-K may promote this event by interacting with TUBB3 and by recruiting at the midbody casein kinase-2alpha (CK2alpha) that has previously been reported to phosphorylate the S444 residue. (PMID:26586574)
• Proper midbody architecture requires cross-regulation between two cell division kinases, Citron kinase (CIT-K) and Aurora B, the kinase component of the chromosomal passenger complex. (PMID:27009191)
• Biallelic Mutations in Citron Kinase Link Mitotic Cytokinesis to Human Primary Microcephaly (PMID:27453578)
• identification of recessively inherited pathogenic variants in CIT as the genetic basis of severe microcephaly and neonatal death; and postmortem data showing that CIT is critical to building a normally sized human brain (PMID:27453579)
• The striking phenotypic overlap between CIT-mutated individuals and the knockout mice and rats that are specifically deficient in the kinase domain supports the proposed causal link between CIT mutation and primary microcephaly in humans. (PMID:27503289)
• Splice site variant in CIT, identified in this study, is predicted to abolish splice donor site. cDNA sequence of an affected individual showed retention of an intron next to the splice donor site. The study, presented here, revealed the first variant in the CIT causing Autosomal recessive primary microcephaly in the family. (PMID:27519304)
• Control of abscission requires Eph kinase activity, and Src and citron kinase (CitK) are downstream effectors in the Eph-induced signal transduction cascade (PMID:27551053)
• in this study we have provided evidence that ASPM controls spindle orientation by regulating the dynamics of astral MT and that CITK is a critical downstream partner of ASPM for this activity. (PMID:27562601)
• CITK deletion decreased tumor growth and increased overall survival in these mice, with no apparent side effects. These results suggest that CITK can be a useful molecular target for medulloblastoma treatment. (PMID:29921697)
• CIT-K overexpression is associated with breast cancer. (PMID:30565087)
• gene expression profile data set showed that MM patients with high CIT gene expression had significantly worse overall survival compared with MM patients with low CIT gene expression. CIT silencing in MM cell lines induced cytokinesis failure and resulted in decreased MM cell proliferation in vitro and in vivo. (PMID:30940634)
• Down-regulation of CIT can inhibit the growth of human bladder cancer cells. (PMID:31972359)
• Novel circRNA_0071196/miRNA19b3p/CIT axis is associated with proliferation and migration of bladder cancer. (PMID:32705161)
• Prostate Cancer Progression Relies on the Mitotic Kinase Citron Kinase. (PMID:37801613)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	citb	ENSDARG00000088825
danio_rerio	cita	ENSDARG00000089856
mus_musculus	Cit	ENSMUSG00000029516
rattus_norvegicus	Cit	ENSRNOG00000001143
drosophila_melanogaster	sti	FBGN0002466

Paralogs (5): ROCK1 (ENSG00000067900), ROCK2 (ENSG00000134318), CDC42BPA (ENSG00000143776), CDC42BPG (ENSG00000171219), CDC42BPB (ENSG00000198752)

Protein

Protein identifiers

Citron Rho-interacting kinase — O14578 (reviewed: O14578)

Alternative names: Serine/threonine-protein kinase 21

All UniProt accessions (12): A0A7I2V2G7, A0A7I2V365, A0A7I2V426, A0A7I2V4A6, A0A7I2V4H7, A0A7I2V4I0, A0A7I2V692, A0A7I2YQJ8, F5H4K4, H0YGG8, H7BYJ3, O14578

UniProt curated annotations — full annotation on UniProt →

Function. Plays a role in cytokinesis. Required for KIF14 localization to the central spindle and midbody. Putative RHO/RAC effector that binds to the GTP-bound forms of RHO and RAC1. It probably binds p21 with a tighter specificity in vivo. Displays serine/threonine protein kinase activity. Plays an important role in the regulation of cytokinesis and the development of the central nervous system. Phosphorylates MYL9/MLC2.

Subunit / interactions. Directly interacts with KIF14 depending on the activation state (stronger interaction with the kinase-dead form). Homodimer. Interacts with TTC3.

Subcellular location. Cytoplasm.

Disease relevance. Microcephaly 17, primary, autosomal recessive (MCPH17) [MIM:617090] A form of microcephaly, a disease defined as a head circumference more than 3 standard deviations below the age, sex and ethnically matched mean. Brain weight is markedly reduced and the cerebral cortex is disproportionately small. MCPH17 is a severe form characterized by lissencephaly, enlarged ventricles, agenesis of the corpus callosum, cerebellar hypoplasia, and brainstem hypoplasia. Patients manifest delayed psychomotor development, intellectual disability, spasticity, axial hypotonia, and dysmorphic features. The disease is caused by variants affecting the gene represented in this entry.

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

Isoforms (4)

UniProt ID	Names	Canonical?
O14578-1	1, Long	yes
O14578-2	2, Short, CRIK-SK
O14578-3	3
O14578-4	4

RefSeq proteins (2): NP_001193928, NP_009105 (=MANE)

Domains & families (InterPro)

ID	Name	Type
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
IPR017405	Citron_Rho-interacting_kinase	Family
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR017892	Pkinase_C	Domain
IPR037708	CRIK_dom	Domain
IPR046349	C1-like_sf	Homologous_superfamily
IPR050839	Rho-assoc_Ser/Thr_Kinase	Family

Pfam: PF00069, PF00169, PF00433, PF00780

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 (44 total): modified residue 10, splice variant 6, sequence variant 6, domain 4, compositionally biased region 4, region of interest 4, sequence conflict 3, binding site 2, chain 1, coiled-coil region 1, short sequence motif 1, active site 1, zinc finger region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O14578-F1	69.75	0.15

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): 221 (proton acceptor)

Ligand- & substrate-binding residues (2): 103–111; 126

Post-translational modifications (10): 1, 433, 440, 480, 582, 1196, 1721, 1940, 1993, 2013

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-5625900	RHO GTPases activate CIT
R-HSA-8980692	RHOA GTPase cycle
R-HSA-9013026	RHOB GTPase cycle
R-HSA-9013106	RHOC GTPase cycle
R-HSA-9013149	RAC1 GTPase cycle

MSigDB gene sets: 349 (showing top): GOBP_MITOTIC_CYTOKINESIS, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOBP_NEUROGENESIS, GOBP_HIPPO_SIGNALING, CACCAGC_MIR138, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_REGULATION_OF_ACTIN_FILAMENT_BASED_PROCESS, PID_RHOA_PATHWAY, CAGCAGG_MIR370, INAMURA_LUNG_CANCER_SCC_SUBTYPES_UP, AAACCAC_MIR140, GOBP_CYTOKINESIS, GOBP_POSITIVE_REGULATION_OF_CELL_DIVISION, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM5, FISCHER_G2_M_CELL_CYCLE

GO Biological Process (11): mitotic cell cycle (GO:0000278), mitotic cytokinesis (GO:0000281), positive regulation of cytokinesis (GO:0032467), regulation of actin cytoskeleton organization (GO:0032956), negative regulation of hippo signaling (GO:0035331), generation of neurons (GO:0048699), neuron apoptotic process (GO:0051402), protein phosphorylation (GO:0006468), nervous system development (GO:0007399), cell differentiation (GO:0030154), cell division (GO:0051301)

GO Molecular Function (16): transcription coactivator binding (GO:0001223), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), zinc ion binding (GO:0008270), SH3 domain binding (GO:0017124), protein kinase binding (GO:0019901), PDZ domain binding (GO:0030165), protein serine/threonine kinase inhibitor activity (GO:0030291), scaffold protein binding (GO:0097110), 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 (3): cytosol (GO:0005829), membrane (GO:0016020), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
RHO GTPase cycle	4
RHO GTPase Effectors	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
protein kinase activity	2
protein domain specific binding	2
cell cycle	1
mitotic nuclear division	1
mitotic cell cycle	1
cytoskeleton-dependent cytokinesis	1
mitotic cell cycle process	1
cytokinesis	1
regulation of cytokinesis	1
positive regulation of cell division	1
positive regulation of cell cycle process	1
actin cytoskeleton organization	1
regulation of actin filament-based process	1
regulation of cytoskeleton organization	1
hippo signaling	1
regulation of hippo signaling	1
negative regulation of intracellular signal transduction	1
neurogenesis	1
apoptotic process	1
phosphorylation	1
protein modification process	1
system development	1
cellular developmental process	1
cellular process	1
transcription coregulator binding	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transition metal ion binding	1
kinase binding	1
protein serine/threonine kinase activity	1
protein kinase inhibitor activity	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

Protein interactions and networks

STRING

3420 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CIT	KIF14	Q15058	905
CIT	KIF20A	O95235	853
CIT	KIF23	Q02241	750
CIT	KIF4A	O95239	747
CIT	KCTD6	Q8NC69	594
CIT	ASPM	Q8IZT6	573
CIT	TTC3	P78477	519
CIT	SPRYD3	Q8NCJ5	501
CIT	CDKN1B	P46527	442
CIT	ANLN	Q9NQW6	442
CIT	PLEK2	Q9NYT0	423
CIT	CCDC60	Q8IWA6	406
CIT	PIP5K1C	O60331	397
CIT	PLEK	P08567	396
CIT	AKT1	P31749	396

IntAct

152 interactions, top by confidence:

A	B	Type	Score
NS	PIK3R2	psi-mi:“MI:0914”(association)	0.750
CIT	TAX1BP3	psi-mi:“MI:0914”(association)	0.690
TAX1BP3	ARVCF	psi-mi:“MI:0914”(association)	0.690
CIT	TAX1BP3	psi-mi:“MI:0407”(direct interaction)	0.690
CIT	SNX27	psi-mi:“MI:0407”(direct interaction)	0.590
CIT	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.590
CIT	MAGI3	psi-mi:“MI:0407”(direct interaction)	0.590
rep	TBKBP1	psi-mi:“MI:0914”(association)	0.530
FRMD5	FAM234B	psi-mi:“MI:0914”(association)	0.530
CIT	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	SCRIB	psi-mi:“MI:0407”(direct interaction)	0.440
PDZD2	CIT	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	SYNJ2BP	psi-mi:“MI:0407”(direct interaction)	0.440
MAST1	CIT	psi-mi:“MI:0407”(direct interaction)	0.440
TAMALIN	CIT	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	ERBIN	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	PATJ	psi-mi:“MI:0407”(direct interaction)	0.440
APBA3	CIT	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	AHNAK	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	APBA2	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	ARHGAP21	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	ARHGEF11	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	CARD11	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	CASK	psi-mi:“MI:0407”(direct interaction)	0.440
CIT	WHRN	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (1505): CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-Western), gag (Affinity Capture-Western), CIT (Two-hybrid), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Affinity Capture-MS), CIT (Positive Genetic), EIF3H (Negative Genetic), ERH (Negative Genetic)

ESM2 similar proteins: A0PJP4, A0PJT0, A2VDP1, A4IFK7, D3ZUQ0, E9PSL7, O14578, O75665, P0C219, P49025, P97817, Q01850, Q0IHE5, Q14BN4, Q17QG3, Q28623, Q3LGD4, Q3SYW5, Q3URD3, Q3V079, Q4R3X1, Q4R7Y8, Q58A65, Q5DTM8, Q5EBL4, Q5R5R4, Q5VTR2, Q5ZJA3, Q5ZLS3, Q62172, Q62796, Q68CZ1, Q6AYA0, Q6DFC2, Q6DH86, Q6NRH3, Q6ZUS6, Q7Z3E2, Q86VS8, Q8BR07

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

7 interactions.

A	Effect	B	Mechanism
KIF14	“up-regulates activity”	CIT	binding
CIT	“up-regulates activity”	KIF14	binding
AURKB	“down-regulates activity”	CIT	phosphorylation
SRC	“up-regulates activity”	CIT	phosphorylation
CIT	“up-regulates activity”	INCENP	phosphorylation
CIT	“up-regulates activity”	MYL9	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 119 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
Ras activation upon Ca2+ influx through NMDA receptor	6	46.3×	3e-07
Unblocking of NMDA receptors, glutamate binding and activation	5	36.7×	2e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	36.7×	2e-05
Assembly and cell surface presentation of NMDA receptors	10	34.3×	7e-11
Dopamine Neurotransmitter Release Cycle	5	33.5×	2e-05
Long-term potentiation	5	32.1×	2e-05
Neurexins and neuroligins	10	26.6×	6e-10
Protein-protein interactions at synapses	6	21.5×	2e-05

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	57.6×	2e-14
receptor clustering	8	45.0×	2e-09
protein localization to synapse	5	34.5×	3e-05
regulation of postsynaptic membrane neurotransmitter receptor levels	7	31.3×	6e-07
establishment of cell polarity	5	17.2×	7e-04
cell-cell adhesion	11	10.1×	2e-06
protein-containing complex assembly	8	8.2×	5e-04
protein transport	11	4.3×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	17
Likely pathogenic	8
Uncertain significance	304
Likely benign	243
Benign	122

Top pathogenic / likely-pathogenic (25)

Variant ID	HGVS	Classification
1333418	NM_001206999.2(CIT):c.957+1G>T	Pathogenic
2104919	NM_001206999.2(CIT):c.3532C>T (p.Arg1178Ter)	Pathogenic
2228558	NM_001206999.2(CIT):c.5515C>T (p.Arg1839Ter)	Pathogenic
252992	NM_001206999.2(CIT):c.1111+1G>A	Pathogenic
252993	NM_001206999.2(CIT):c.412C>T (p.Gln138Ter)	Pathogenic
252994	NM_001206999.2(CIT):c.473C>G (p.Pro158Arg)	Pathogenic
254134	NM_001206999.2(CIT):c.317G>T (p.Gly106Val)	Pathogenic
254135	NM_001206999.2(CIT):c.376A>C (p.Lys126Gln)	Pathogenic
254136	NM_001206999.2(CIT):c.689A>T (p.Asp230Val)	Pathogenic
254139	NM_001206999.2(CIT):c.753+3A>T	Pathogenic
2835069	NM_001206999.2(CIT):c.1220C>G (p.Ser407Ter)	Pathogenic
2895340	NM_001206999.2(CIT):c.1189del (p.Val397fs)	Pathogenic
4537236	NC_000012.11:g.(120288080_120295326)_(120295503_120306863)del	Pathogenic
4697884	NM_001206999.2(CIT):c.426dup (p.Glu143Ter)	Pathogenic
4721274	NM_001206999.2(CIT):c.613del (p.Glu204_Leu205insTer)	Pathogenic
871735	NM_001206999.2(CIT):c.658C>T (p.Arg220Ter)	Pathogenic
983220	NM_001206999.2(CIT):c.4617del (p.Asp1541fs)	Pathogenic
221283	NM_001206999.2(CIT):c.29_38del (p.Asn10fs)	Likely pathogenic
3017974	NM_001206999.2(CIT):c.517-1G>C	Likely pathogenic
3234970	NM_001206999.2(CIT):c.1555C>T (p.Arg519Ter)	Likely pathogenic
3643476	NM_001206999.2(CIT):c.958-1G>A	Likely pathogenic
3643863	NM_001206999.2(CIT):c.97-2A>T	Likely pathogenic
377365	NM_001206999.2(CIT):c.1122dup (p.Phe375fs)	Likely pathogenic
871734	NM_001206999.2(CIT):c.1070A>G (p.His357Arg)	Likely pathogenic
983219	NM_001206999.2(CIT):c.367T>G (p.Tyr123Asp)	Likely pathogenic

SpliceAI

7783 predictions. Top by Δscore:

Variant	Effect	Δscore
12:119690148:CACC:C	donor_loss	1.0000
12:119690149:A:T	donor_loss	1.0000
12:119698087:C:CT	acceptor_gain	1.0000
12:119700741:GTAC:G	donor_loss	1.0000
12:119700742:TACCA:T	donor_loss	1.0000
12:119700743:A:AC	donor_gain	1.0000
12:119700743:ACCAA:A	donor_loss	1.0000
12:119700744:C:CA	donor_loss	1.0000
12:119700744:C:CC	donor_gain	1.0000
12:119700826:C:CC	acceptor_gain	1.0000
12:119701617:GACTC:G	donor_loss	1.0000
12:119701618:ACTCA:A	donor_loss	1.0000
12:119701620:TCA:T	donor_loss	1.0000
12:119701621:CAC:C	donor_loss	1.0000
12:119701622:A:AC	donor_gain	1.0000
12:119701623:C:CC	donor_gain	1.0000
12:119701753:C:CC	acceptor_gain	1.0000
12:119701848:AC:A	donor_gain	1.0000
12:119701849:CC:C	donor_gain	1.0000
12:119701956:CTC:C	acceptor_gain	1.0000
12:119701959:C:CA	acceptor_loss	1.0000
12:119701965:CA:C	acceptor_gain	1.0000
12:119701966:A:C	acceptor_gain	1.0000
12:119704359:TTA:T	donor_loss	1.0000
12:119704360:TACTT:T	donor_loss	1.0000
12:119704361:A:AC	donor_gain	1.0000
12:119704361:ACTTT:A	donor_gain	1.0000
12:119704362:C:CG	donor_gain	1.0000
12:119704362:CT:C	donor_gain	1.0000
12:119704362:CTT:C	donor_gain	1.0000

AlphaMissense

13637 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:119697716:C:T	G1900E	1.000
12:119697717:C:G	G1900R	1.000
12:119697717:C:T	G1900R	1.000
12:119697765:A:C	Y1884D	1.000
12:119697785:G:T	A1877D	1.000
12:119697791:C:A	G1875V	1.000
12:119697791:C:T	G1875D	1.000
12:119697792:C:G	G1875R	1.000
12:119698012:A:G	L1847P	1.000
12:119698033:A:G	F1840S	1.000
12:119698036:A:G	L1839P	1.000
12:119698040:A:C	Y1838D	1.000
12:119700769:A:G	W1825R	1.000
12:119700769:A:T	W1825R	1.000
12:119700798:C:A	G1815V	1.000
12:119700798:C:T	G1815E	1.000
12:119700819:C:T	G1808E	1.000
12:119700820:C:G	G1808R	1.000
12:119700820:C:T	G1808R	1.000
12:119701897:C:T	G1747E	1.000
12:119701898:C:G	G1747R	1.000
12:119701898:C:T	G1747R	1.000
12:119704403:A:G	L1713P	1.000
12:119704427:G:T	A1705D	1.000
12:119708202:A:G	C1688R	1.000
12:119710349:A:G	L1616P	1.000
12:119710362:C:A	G1612W	1.000
12:119710373:C:T	G1608D	1.000
12:119710374:C:G	G1608R	1.000
12:119710610:C:T	G1580E	1.000

dbSNP variants (sampled 300 via entrez): RS1000008060 (12:119872075 C>T), RS1000017115 (12:119843758 C>A,T), RS1000047208 (12:119705056 G>A), RS1000052517 (12:119704833 A>C), RS1000081350 (12:119872604 A>G), RS1000089869 (12:119782442 C>T), RS1000093941 (12:119791673 G>A), RS1000121816 (12:119756294 G>A,C), RS1000126547 (12:119791977 G>A), RS1000138274 (12:119747577 G>A), RS1000201394 (12:119866671 T>C,G), RS1000221286 (12:119830635 G>C), RS1000237324 (12:119687099 T>C), RS1000244241 (12:119829183 C>T), RS1000257029 (12:119741429 T>C)

Disease associations

OMIM: gene MIM:605629 | disease phenotypes: MIM:617090, MIM:251200

GenCC curated gene-disease

Disease	Classification	Inheritance
microcephaly 17, primary, autosomal recessive	Strong	Autosomal recessive
autosomal recessive primary microcephaly	Supportive	Autosomal recessive

Mondo (4): microcephaly 17, primary, autosomal recessive (MONDO:0014908), long QT syndrome (MONDO:0002442), autosomal recessive primary microcephaly (MONDO:0016660), intellectual disability (MONDO:0001071)

Orphanet (2): Autosomal recessive primary microcephaly (Orphanet:2512), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

40 total (30 of 40 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000076	Vesicoureteral reflux
HP:0000104	Renal agenesis
HP:0000122	Unilateral renal agenesis
HP:0000219	Thin upper lip vermilion
HP:0000252	Microcephaly
HP:0000294	Low anterior hairline
HP:0000316	Hypertelorism
HP:0000340	Sloping forehead
HP:0000400	Macrotia
HP:0000414	Bulbous nose
HP:0000582	Upslanted palpebral fissure
HP:0000750	Delayed speech and language development
HP:0001249	Intellectual disability
HP:0001250	Seizure
HP:0001257	Spasticity
HP:0001263	Global developmental delay
HP:0001274	Agenesis of corpus callosum
HP:0001276	Hypertonia
HP:0001302	Pachygyria
HP:0001321	Cerebellar hypoplasia
HP:0001347	Hyperreflexia
HP:0001508	Failure to thrive
HP:0001510	Growth delay
HP:0002079	Hypoplasia of the corpus callosum
HP:0002119	Ventriculomegaly
HP:0002194	Delayed gross motor development
HP:0002282	Gray matter heterotopia
HP:0002365	Hypoplasia of the brainstem
HP:0003103	Abnormal cortical bone morphology

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST002723_6	Urgency urinary incontinence	9.000000e-07
GCST007326_51	Number of sexual partners	2.000000e-09
GCST011878_18	Mitochondrial heteroplasmy measurement	1.000000e-08

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0006865	urgency urinary incontinence
EFO:0600008	mitochondrial heteroplasmy measurement

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D008133	Long QT Syndrome	C14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547
C579935	Autosomal Recessive Primary Microcephaly (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5579 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

41 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 565,775 (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
CHEMBL1078178	MOMELOTINIB	4	3,481
CHEMBL1173655	AFATINIB	4	15,144
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL1789941	RUXOLITINIB	4	11,547
CHEMBL2105759	BARICITINIB	4	6,741
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL535	SUNITINIB	4	79,020
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL939	GEFITINIB	4	117,814
CHEMBL101253	VATALANIB	3	11,319
CHEMBL2219422	AFURESERTIB	3	1,467
CHEMBL31965	CANERTINIB	3	8,083
CHEMBL38380	FASUDIL	3	11,953
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL572881	MOTESANIB	3	4,642
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3
CHEMBL103667	DORAMAPIMOD	2
CHEMBL1230609	FORETINIB	2
CHEMBL1721885	SU-014813	2
CHEMBL215152	DEFOSBARASERTIB	2
CHEMBL3545396	BMS-690514	2
CHEMBL475251	R-406	2
CHEMBL5089410	PILAVAPADIN	2
CHEMBL513909	BI-2536	2

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Other DMPK family kinases

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
C3TD879	Inhibition	7.92	pIC50

Binding affinities (BindingDB)

185 measured of 185 human assays (185 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea	KD	0.37 nM
Staurosporine	KD	1.7 nM
(2R)-2-Amino-N-[4-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-4,4-dimethyl-pentanamide	IC50	4 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R,3S)-2-amino-3-hydroxy-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	5 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-4,4-dimethyl-N-[3-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	7.8 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[3-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	8.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[6-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-2-methoxy-3-pyridyl]-4,4-dimethyl-pentanamide	IC50	9 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-4,4-dimethyl-N-[4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	9.1 nM	US-20250243196: CITRON KINASE INHIBITORS
4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole	KD	9.8 nM
(2R)-2-Amino-N-[4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4,4-dimethyl-pentanamide	IC50	10 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-fluoro-3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4,4-dimethyl-pentanamide	IC50	10 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-3-cyclopentyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	IC50	10.4 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[4-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-3-methyl-phenyl]-4,4-dimethyl-pentanamide	IC50	11.7 nM	US-20250243196: CITRON KINASE INHIBITORS
4-[4-(4-fluorophenyl)-2-(4-methanesulfinylphenyl)-1H-imidazol-5-yl]pyridine	KD	12 nM
(2R)-2-amino-4,4-dimethyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	12 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	12.5 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4,4-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	13.8 nM	US-20250243196: CITRON KINASE INHIBITORS
2-Amino-4,4-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	14.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-N-[4-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-4-methylpentanamide	IC50	16.8 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-fluoro-3-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methyl-pentanamide	IC50	17 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-N-[3-ethyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	IC50	17.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-3-methyl-phenyl]-4,4-dimethyl-pentanamide	IC50	18 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-methoxy-6-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-3-pyridyl]-4,4-dimethyl-pentanamide	IC50	18 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[4-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-3-methyl-phenyl]-4-methyl-pentanamide	IC50	18.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	18.8 nM	US-20250243196: CITRON KINASE INHIBITORS
(2S,3R)-2-amino-3-hydroxy-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	19 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-3,3-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]butanamide	IC50	19.6 nM	US-20250243196: CITRON KINASE INHIBITORS
(R)-2-Amino-N-(3-(difluoromethoxy)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl)-4-methylpentanamide	IC50	21.5 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	21.9 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4,4-dimethyl-N-[4-[2-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]pentanamide	IC50	22 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-4-methyl-2-(methylamino)-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	22.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-fluoro-3-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-3,3-dimethyl-butanamide	IC50	23.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-fluoro-3-methyl-4-[2-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-4,4-dimethyl-pentanamide	IC50	24 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-4,4-dimethyl-N-(6-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)pyridin-3-yl)pentanamide	IC50	26 nM	US-20250243196: CITRON KINASE INHIBITORS
2-Amino-3-hydroxy-4,4-dimethyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	IC50	29 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[3-(difluoromethyl)-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4,4-dimethyl-pentanamide	IC50	29.3 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-3,3-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiazol-2-yl]butanamide	IC50	29.6 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-4-methyl-N-[3-methyl-4-[2-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]pentanamide	IC50	30.4 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-5-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]hexanamide	IC50	30.6 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-N-[3-(difluoromethyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	IC50	31.3 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[6-methoxy-5-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)-2-pyridyl]-4,4-dimethyl-pentanamide	IC50	35 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-3,3-dimethyl-butanamide	IC50	35.1 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-3-(trifluoromethoxy)phenyl]pentanamide	IC50	36.9 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methyl-pentanamide	IC50	36.9 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[3-methoxy-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4,4-dimethyl-pentanamide	IC50	37 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	IC50	37.5 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-Amino-N-[2-methoxy-6-[2-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-3-pyridyl]-4,4-dimethyl-pentanamide	IC50	38 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-N-[2-methoxy-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	IC50	39.3 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-3-(3-hydroxyphenyl)-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	IC50	39.6 nM	US-20250243196: CITRON KINASE INHIBITORS
(2R)-2-amino-4-methyl-N-[6-(1H-pyrrolo[2,3-b]pyridin-4-yl)-3-pyridinyl]pentanamide	IC50	39.8 nM	US-20250243196: CITRON KINASE INHIBITORS

ChEMBL bioactivities

156 potent at pChembl≥5 of 160 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.52	Kd	0.3	nM	CHEMBL5572737
8.52	Kd	3	nM	CHEMBL400402
8.26	IC50	5.5	nM	CHEMBL5591534
8.02	Kd	9.5	nM	CHEMBL5572737
8.00	IC50	10	nM	CHEMBL5568742
7.92	IC50	12	nM	CHEMBL5572737
7.89	IC50	13	nM	CHEMBL5595104
7.89	Kd	13	nM	CHEMBL379218
7.85	IC50	14	nM	CHEMBL5575901
7.82	IC50	15	nM	CHEMBL5569359
7.80	IC50	16	nM	CHEMBL5579704
7.80	IC50	16	nM	CHEMBL5575300
7.77	IC50	17	nM	CHEMBL5590268
7.77	IC50	17	nM	CHEMBL5595678
7.75	IC50	18	nM	CHEMBL5575657
7.70	IC50	20	nM	CHEMBL5574799
7.68	IC50	21	nM	CHEMBL5566667
7.51	IC50	31	nM	CHEMBL5562828
7.51	IC50	31	nM	CHEMBL5566783
7.48	Kd	33	nM	Y-39983
7.43	IC50	37	nM	CHEMBL5542511
7.43	IC50	37	nM	CHEMBL5574511
7.41	IC50	39	nM	CHEMBL5573191
7.40	IC50	40	nM	CHEMBL5571250
7.40	IC50	40	nM	CHEMBL5571047
7.40	IC50	40	nM	CHEMBL5574143
7.40	IC50	40	nM	CHEMBL5563128
7.38	IC50	42	nM	CHEMBL5572919
7.32	IC50	48	nM	CHEMBL5563995
7.29	IC50	51	nM	CHEMBL5572737
7.28	Kd	52	nM	AST-487
7.27	IC50	54	nM	CHEMBL5574850
7.25	IC50	56	nM	CHEMBL5088205
7.22	IC50	60	nM	CHEMBL5195653
7.21	IC50	61	nM	CHEMBL5570381
7.18	IC50	66	nM	CHEMBL5590500
7.17	IC50	67	nM	CHEMBL5574584
7.10	IC50	80	nM	CHEMBL5566515
7.07	Kd	85	nM	LESTAURTINIB
7.06	Kd	87	nM	RAF-265
7.05	IC50	90	nM	CHEMBL5205578
7.05	IC50	90	nM	CHEMBL5571741
7.05	IC50	89	nM	CHEMBL5566014
7.04	IC50	92	nM	CHEMBL5572680
7.03	Kd	94	nM	SU-014813
7.01	Kd	98	nM	CHEMBL3688339
6.96	IC50	110	nM	CHEMBL5590585
6.96	IC50	110	nM	CHEMBL5575031
6.96	Kd	110	nM	ALVOCIDIB
6.92	IC50	120	nM	CHEMBL4872886

PubChem BioAssay actives

150 with measured affinity, of 559 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
(2R)-2-amino-4,4-dimethyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100169: Binding affinity to NanoLuc fused-CITK kinase domain (unknown origin) expressed in HEK293T cells assessed as dissociation constant NanoBRET Target Engagement Intracellular Kinase Assay	kd	0.0003	uM
4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenol	1424954: 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	0.0030	uM
(2R,3S)-2-amino-3-hydroxy-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0055	uM
(2R)-2-amino-3-cyclopentyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0100	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	625065: Binding constant for CIT kinase domain	kd	0.0130	uM
(2R)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0130	uM
(2R)-2-amino-4,4-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0140	uM
(2R)-2-amino-4-methyl-N-[3-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0150	uM
(2S,3R)-2-amino-3-hydroxy-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0160	uM
(2R)-2-amino-3,3-dimethyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]butanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0160	uM
(2R)-2-amino-N-[3-ethyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0170	uM
(2R)-2-amino-N-[4-[2-(difluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0170	uM
(2R)-2-amino-4-methyl-N-[3-methyl-4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0180	uM
(2R)-2-amino-4-methyl-N-[4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0200	uM
(2R)-4-methyl-2-(methylamino)-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0210	uM
(2R)-2-amino-5-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]hexanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0310	uM
(2R)-2-amino-N-[3-(difluoromethyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0310	uM
4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide	1424954: 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	0.0330	uM
(2R)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-3-(trifluoromethoxy)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0370	uM
(2R)-2-amino-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0370	uM
(2R)-2-amino-N-[4-(2-amino-4-pyridinyl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0390	uM
(2R)-2-amino-N-[2-methoxy-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0400	uM
(2R)-2-amino-4-methyl-N-[6-(1H-pyrrolo[2,3-b]pyridin-4-yl)-3-pyridinyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0400	uM
(2R)-2-amino-3-phenyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0400	uM
(2R)-2-amino-3-(3-hydroxyphenyl)-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0400	uM
(2S)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0420	uM
(2R)-2-amino-N-[4-(2-cyclopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0480	uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea	435523: Binding constant for CIT kinase domain	kd	0.0520	uM
(2R)-2-amino-4-methyl-N-[4-[2-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0540	uM
(2S)-1-[2-(difluoromethyl)-4-[2-(difluoromethyl)-4-pyridinyl]phenoxy]-2,4-dimethylpentan-2-amine	1826907: Inhibition of CRIK (unknown origin)	ic50	0.0560	uM
methyl N-[4-[5-[(2S)-2-amino-2,4-dimethylpentoxy]-4-methyl-2-pyridinyl]-2-pyridinyl]carbamate	1904671: Inhibition of CRIK (unknown origin)	ic50	0.0600	uM
(2R)-2-amino-3-cyclobutyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0610	uM
(2R)-2-amino-3-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]butanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0660	uM
(2R)-2-amino-4-methyl-N-[4-(5-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0670	uM
(2R)-2-amino-N-[2-chloro-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0800	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	507876: Binding affinity to CIT	kd	0.0850	uM
1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine	435523: Binding constant for CIT kinase domain	kd	0.0870	uM
(2R)-2-amino-N-[3-cyano-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0890	uM
methyl N-[4-[5-[(2S)-2-amino-2,4-dimethylpentoxy]-6-chloro-2-pyridinyl]-2-pyridinyl]carbamate	1904671: Inhibition of CRIK (unknown origin)	ic50	0.0900	uM
(2R)-2-amino-3-(3-methoxyphenyl)-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]propanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0900	uM
(2R)-2-amino-4-methyl-N-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1,3-thiazol-2-yl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.0920	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	435523: Binding constant for CIT kinase domain	kd	0.0940	uM
1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone	1424954: 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	0.0980	uM
(2R)-2-amino-N-[3-methoxy-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]-4-methylpentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.1100	uM
(2R)-2-amino-4-methyl-N-[6-methyl-5-(1H-pyrrolo[2,3-b]pyridin-4-yl)-2-pyridinyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.1100	uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one	435523: Binding constant for CIT kinase domain	kd	0.1100	uM
(2R)-2-amino-N-[3-(difluoromethoxy)-4-(1,3-oxazol-5-yl)phenyl]-4-methylpentanamide	1769868: Inhibition of CRIK (unknown origin) by Kinomescan method	ic50	0.1200	uM
(2R)-2-amino-4-methyl-N-[2-methyl-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl]pentanamide	2100129: Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay	ic50	0.1300	uM
Fedratinib	625065: Binding constant for CIT kinase domain	kd	0.1400	uM
2-[3-(methanesulfonamido)phenyl]-N-[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-1,3-thiazol-2-yl]acetamide	1398865: Inhibition of CIT (unknown origin)	ki	0.1600	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, increases methylation	5
Benzo(a)pyrene	decreases expression	3
Resveratrol	affects cotreatment, increases expression, decreases expression	2
Acetaminophen	decreases expression, increases expression	2
Arsenic	affects methylation, decreases methylation, increases abundance	2
Methotrexate	affects cotreatment, decreases expression, increases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	decreases expression, increases expression	2
Cyclosporine	decreases expression	2
Aflatoxin B1	affects expression, increases methylation	2
FR900359	decreases phosphorylation	1
dicrotophos	increases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	decreases expression	1
bisphenol A	decreases methylation	1
geraniol	decreases expression	1
titanium dioxide	decreases methylation	1
arsenite	affects binding, decreases reaction	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
sodium arsenite	increases expression	1
cobaltous chloride	decreases expression	1
butyraldehyde	decreases expression	1
perfluorooctanoic acid	decreases expression	1
zinc chromate	decreases expression, increases abundance	1
benzo(e)pyrene	increases methylation	1
aflatoxin B2	decreases methylation	1
coumarin	decreases phosphorylation	1
cupric oxide	decreases expression	1
diallyl trisulfide	decreases expression	1
pentanal	decreases expression	1

ChEMBL screening assays

145 unique, capped per target: 145 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1032272	Binding	Inhibition of CIT at 3 uM	Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2UF	Abcam HEK293T CIT KO	Transformed cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT02513940	PHASE4	COMPLETED	Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes
NCT03834883	PHASE4	COMPLETED	Reducing the Risk of Drug-Induced QT Interval Lengthening in Women
NCT04169100	PHASE4	UNKNOWN	Novel Form of Acquired Long QT Syndrome
NCT04675788	PHASE4	COMPLETED	Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening
NCT05657860	PHASE4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	PHASE4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	PHASE4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	PHASE4	NOT_YET_RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT02270736	PHASE3	COMPLETED	Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT01648205	PHASE2	COMPLETED	Long-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients
NCT02412709	PHASE2	UNKNOWN	Long QT Syndrome Screening in Newborns
NCT04581408	PHASE2	COMPLETED	Mutation-specific Therapy for the Long QT Syndrome
NCT02304302	PHASE2	COMPLETED	Down Syndrome Memantine Follow-up Study
NCT03862950	PHASE2	COMPLETED	A Trial of Metformin in Individuals With Fragile X Syndrome (Met)
NCT04529226	PHASE2	UNKNOWN	Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis
NCT04821856	PHASE2	COMPLETED	Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability
NCT00316459	PHASE1	COMPLETED	Study Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects
NCT01849003	PHASE1	COMPLETED	Study of the Effect of GS-6615 in Subjects With LQT-3
NCT02365532	PHASE1	COMPLETED	Effect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults
NCT02412098	PHASE1	COMPLETED	Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function
NCT02441829	PHASE1	COMPLETED	Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function
NCT05759962	PHASE1	COMPLETED	Phase 1 Study of LQT-1213 in Healthy Adults
NCT05273320	PHASE1	COMPLETED	Clinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities
NCT05301361	PHASE1	ENROLLING_BY_INVITATION	Sensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities
NCT06016764	PHASE1	COMPLETED	Use of MRI and cTBS for Catatonia in Autism
NCT06586827	PHASE1	COMPLETED	Impact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD
NCT07531940	PHASE1	NOT_YET_RECRUITING	Escalating Doses of Memantine in Down Syndrome (MEDS-123)
NCT05906732	PHASE1/PHASE2	TERMINATED	Study of LQT-1213 on QTc-induced Prolongation in Healthy Adult Subjects (Part1) and on Congenital Long QT in Patients Diagnosed With Type 2 or 3 Long QT Syndrome (Part 2).
NCT00005176	Not specified	COMPLETED	Long QT Syndrome-Population Genetics and Cardiac Studies
NCT00005250	Not specified	COMPLETED	Linkage Study of Long QT Syndrome In An Amish Kindred
NCT00005367	Not specified	COMPLETED	Epidemiology of Long QTand Asian Sudden Death in Sleep
NCT00221832	Not specified	UNKNOWN	Molecular Genetic Screening and Identification of Congenital Arrhythmogenic Diseases
NCT00292032	Not specified	COMPLETED	Registry of Unexplained Cardiac Arrest
NCT00335036	Not specified	TERMINATED	Pediatric Lead Extractability and Survival Evaluation (PLEASE)
NCT00399412	Not specified	COMPLETED	ECG Signal Collection From Long QT Syndrome, Wide QRS Complexes, Heart Failure, and Cardiac Resynchronization Patients
NCT00488254	Not specified	COMPLETED	The Long QT Syndrome in Pregnancy
NCT00588965	Not specified	COMPLETED	Effect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects
NCT01705925	Not specified	COMPLETED	Multicenter Evaluation of Children and Young Adults With Genotype Positive Long QT Syndrome
NCT01903564	Not specified	COMPLETED	Fetal and Neonatal Magnetophysiology
NCT02082431	Not specified	COMPLETED	Determine the Incidence of Long QT Amongst a Large Cohort of Subjects Diagnosed With Unilateral or Bilateral Sensorineural Hearing Loss.