CKMT1B

Summary

CKMT1B (creatine kinase, mitochondrial 1B, HGNC:1995) is a protein-coding gene on chromosome 15q15.3, encoding Creatine kinase U-type, mitochondrial (P12532). Reversibly catalyzes the transfer of phosphate between ATP and various phosphogens (e.g. creatine phosphate).

Mitochondrial creatine (MtCK) kinase is responsible for the transfer of high energy phosphate from mitochondria to the cytosolic carrier, creatine. It belongs to the creatine kinase isoenzyme family. It exists as two isoenzymes, sarcomeric MtCK and ubiquitous MtCK, encoded by separate genes. Mitochondrial creatine kinase occurs in two different oligomeric forms: dimers and octamers, in contrast to the exclusively dimeric cytosolic creatine kinase isoenzymes. Many malignant cancers with poor prognosis have shown overexpression of ubiquitous mitochondrial creatine kinase; this may be related to high energy turnover and failure to eliminate cancer cells via apoptosis. Ubiquitous mitochondrial creatine kinase has 80% homology with the coding exons of sarcomeric mitochondrial creatine kinase. Two genes located near each other on chromosome 15 have been identified which encode identical mitochondrial creatine kinase proteins.

Source: NCBI Gene 1159 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 29 total — 5 pathogenic
• Druggable target: yes
• MANE Select transcript: NM_001375484

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1995
Approved symbol	CKMT1B
Name	creatine kinase, mitochondrial 1B
Location	15q15.3
Locus type	gene with protein product
Status	Approved
Aliases	UMTCK
Ensembl gene	ENSG00000237289
Ensembl biotype	protein_coding
OMIM	123290
Entrez	1159

Gene structure

Transcript identifiers

Ensembl transcripts: 26 — 19 protein_coding, 4 protein_coding_CDS_not_defined, 2 nonsense_mediated_decay, 1 retained_intron

ENST00000300283, ENST00000411560, ENST00000417289, ENST00000428981, ENST00000437534, ENST00000437924, ENST00000441322, ENST00000449946, ENST00000453733, ENST00000453782, ENST00000475589, ENST00000481666, ENST00000495545, ENST00000498538, ENST00000627381, ENST00000882064, ENST00000882065, ENST00000882066, ENST00000882067, ENST00000882068, ENST00000934243, ENST00000934244, ENST00000934245, ENST00000934246, ENST00000941988, ENST00000941989

RefSeq mRNA: 2 — MANE Select: NM_001375484 NM_001375484, NM_020990

CCDS: CCDS10097

Canonical transcript exons

ENST00000441322 — 9 exons

Exon	Start	End
ENSE00001696702	43598193	43598327
ENSE00001698200	43596408	43596531
ENSE00001764477	43596207	43596292
ENSE00001796028	43595856	43596077
ENSE00003531055	43595374	43595469
ENSE00003537642	43594972	43595170
ENSE00003551403	43598827	43598952
ENSE00003899750	43599157	43599406
ENSE00003903488	43594027	43594367

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 99.47.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right hemisphere of cerebellum	UBERON:0014890	99.47	gold quality
cerebellar hemisphere	UBERON:0002245	99.45	gold quality
cerebellar cortex	UBERON:0002129	99.44	gold quality
cerebellum	UBERON:0002037	99.43	gold quality
mucosa of transverse colon	UBERON:0004991	98.75	gold quality
primary visual cortex	UBERON:0002436	97.91	gold quality
duodenum	UBERON:0002114	97.49	gold quality
rectum	UBERON:0001052	97.27	gold quality
superior frontal gyrus	UBERON:0002661	97.11	gold quality
right frontal lobe	UBERON:0002810	96.95	gold quality
Brodmann (1909) area 9	UBERON:0013540	96.82	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	96.55	gold quality
frontal cortex	UBERON:0001870	95.77	gold quality
frontal lobe	UBERON:0016525	95.77	gold quality
esophagus mucosa	UBERON:0002469	95.47	gold quality
anterior cingulate cortex	UBERON:0009835	94.87	gold quality
prefrontal cortex	UBERON:0000451	94.84	gold quality
cerebral cortex	UBERON:0000956	94.81	gold quality
nucleus accumbens	UBERON:0001882	94.43	gold quality
telencephalon	UBERON:0001893	94.00	gold quality
hypothalamus	UBERON:0001898	93.81	gold quality
brain	UBERON:0000955	93.50	gold quality
putamen	UBERON:0001874	93.36	gold quality
caudate nucleus	UBERON:0001873	92.68	gold quality
lower esophagus mucosa	UBERON:0035834	92.65	gold quality
Ammon’s horn	UBERON:0001954	91.95	gold quality
skin of abdomen	UBERON:0001416	91.80	gold quality
temporal lobe	UBERON:0001871	91.63	gold quality
amygdala	UBERON:0001876	91.56	gold quality
zone of skin	UBERON:0000014	91.06	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-GEOD-86618	yes	122.09
E-ANND-3	yes	11.42

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

11 targeting CKMT1B, 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-4534	99.99	66.58	1907
HSA-MIR-3612	99.45	66.02	1333
HSA-MIR-650	99.45	65.77	1309
HSA-MIR-6722-3P	99.45	67.62	1919
HSA-MIR-2392	99.43	67.50	708
HSA-MIR-1909-3P	99.03	66.56	1662
HSA-MIR-1207-3P	98.99	66.22	1532
HSA-MIR-4443	98.02	66.25	1928
HSA-MIR-4294	97.86	65.72	1110
HSA-MIR-4529-5P	96.74	65.77	569
HSA-MIR-6508-3P	96.73	65.48	576

Literature-anchored findings (GeneRIF, showing 10)

• Significantly greater creatine kinase carbonylation is associated with chronic obstructive pulmonary disease (PMID:16166745)
• Because creatine kinase temporally buffers ATP, these observations support the hypothesis that a deficit in myofibrillar energy delivery contributes to chronic heart failure pathophysiology in human left ventricular hypertrophy. (PMID:16952984)
• LRRK2 can interact directly with uMtCK to block its entry into mitochondria and its subsequent processing. (PMID:21370995)
• The results indicated that uMtCK expression is associated with a poor prognosis in breast cancer and might serve as a tumor marker. (PMID:22982673)
• mitochondrial creatine kinase expression in hepatocellular carcinoma may be caused by hepatocarcinogenesis per se but not by loss of mitochondrial integrity, of which ASB9 could be a negative regulator (PMID:24174293)
• CKMT1 is a key regulator of the permeability transition pore through a complex that is distinct from the classical permeability transition pore. (PMID:24522192)
• The highly conserved residue E227 acts as the catalytic base to accept the guanidinium proton transferred from creatine in UMTCK. (PMID:27909311)
• Mitochondrial creatine kinase CKMT1 is necessary for survival of EVI1-expressing cells in subjects with EVI1-positive AML. (PMID:28191887)
• CKMT1B is a potential prognostic biomarker and associated with immune infiltration in Lower-grade glioma. (PMID:33465115)
• Context-dependent roles for ubiquitous mitochondrial creatine kinase CKMT1 in breast cancer progression. (PMID:38615320)

Cross-species orthologs

12 orthologs

Organism	Symbol	Gene ID
danio_rerio	ckmt1	ENSDARG00000016598
mus_musculus	Ckmt1	ENSMUSG00000000308
rattus_norvegicus	Ckmt1	ENSRNOG00000014573
drosophila_melanogaster	Argk1	FBGN0000116
drosophila_melanogaster	Argk2	FBGN0035957
drosophila_melanogaster	CG4546	FBGN0038373
drosophila_melanogaster	CG30274	FBGN0050274
caenorhabditis_elegans		WBGENE00009706
caenorhabditis_elegans	ZC434.8	WBGENE00013894
caenorhabditis_elegans	F32B5.1	WBGENE00017975
caenorhabditis_elegans		WBGENE00018519
caenorhabditis_elegans	W10C8.5	WBGENE00021128

Paralogs (4): CKM (ENSG00000104879), CKMT2 (ENSG00000131730), CKB (ENSG00000166165), CKMT1A (ENSG00000223572)

Protein

Protein identifiers

Creatine kinase U-type, mitochondrial — P12532 (reviewed: P12532)

Alternative names: Acidic-type mitochondrial creatine kinase, Ubiquitous mitochondrial creatine kinase

All UniProt accessions (8): P12532, C9J6W7, C9J995, C9JFS8, C9JJX8, C9JSQ1, F8WCN3, F8WFC7

UniProt curated annotations — full annotation on UniProt →

Function. Reversibly catalyzes the transfer of phosphate between ATP and various phosphogens (e.g. creatine phosphate). Creatine kinase isoenzymes play a central role in energy transduction in tissues with large, fluctuating energy demands, such as skeletal muscle, heart, brain and spermatozoa.

Subunit / interactions. Exists as an octamer composed of four MTCK homodimers.

Subcellular location. Mitochondrion inner membrane.

Miscellaneous. Mitochondrial creatine kinase binds cardiolipin.

Similarity. Belongs to the ATP:guanido phosphotransferase family.

Isoforms (2)

UniProt ID	Names	Canonical?
P12532-1	1	yes
P12532-2	2

RefSeq proteins (2): NP_001362413, NP_066270 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000749	ATP-guanido_PTrfase	Family
IPR014746	Gln_synth/guanido_kin_cat_dom	Homologous_superfamily
IPR022413	ATP-guanido_PTrfase_N	Domain
IPR022414	ATP-guanido_PTrfase_cat	Domain
IPR022415	ATP-guanido_PTrfase_AS	Active_site
IPR036802	ATP-guanido_PTrfase_N_sf	Homologous_superfamily

Pfam: PF00217, PF02807

Enzyme classification (BRENDA):

• EC 2.7.3.2 — creatine kinase (BRENDA: 45 organisms, 67 substrates, 117 inhibitors, 317 Km, 122 kcat entries)

Substrate kinetics (BRENDA)

10 substrates with measured Km, best-characterized 10. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.042–20	133
CREATINE	0.35–167	102
PHOSPHOCREATINE	0.51–8.97	23
ADP	0.015–1.2	22
CREATINE PHOSPHATE	0.23–50	11
ALPHA-(RP)-BORANO SUBSTITUTED ADP	1	1
ALPHA-(SP)-BORANO SUBSTITUTED ADP	0.008	1
GLYCOCYAMINE	6.7	1
CYCLOCREATINE	—	0
N-ETHYLGLYCOCYAMINE	—	0

Catalyzed reactions (Rhea), 1 shown:

• creatine + ATP = N-phosphocreatine + ADP + H(+) (RHEA:17157)

UniProt features (55 total): helix 17, strand 13, binding site 6, turn 6, modified residue 5, sequence conflict 2, domain 2, transit peptide 1, chain 1, splice variant 1, region of interest 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
9B14	ELECTRON MICROSCOPY	2.2
9B0T	ELECTRON MICROSCOPY	2.3
9B05	ELECTRON MICROSCOPY	2.4
9B0U	ELECTRON MICROSCOPY	2.44
9B04	ELECTRON MICROSCOPY	2.52
9Z2F	ELECTRON MICROSCOPY	2.59
9Z2D	ELECTRON MICROSCOPY	2.6
1QK1	X-RAY DIFFRACTION	2.7
9B16	ELECTRON MICROSCOPY	2.89

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P12532-F1	89.88	0.80

Functional residue map

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

Ligand- & substrate-binding residues (6): 368; 161–165; 224; 269; 325; 353–358

Post-translational modifications (5): 151, 196, 213, 232, 355

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-71288	Creatine metabolism
R-HSA-1430728	Metabolism
R-HSA-71291	Metabolism of amino acids and derivatives

MSigDB gene sets: 122 (showing top): JAEGER_METASTASIS_DN, ENK_UV_RESPONSE_KERATINOCYTE_UP, SP3_Q3, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, TGACCTY_ERR1_Q2, GGGTGGRR_PAX4_03, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, MODULE_66, TCF4_Q5, RICKMAN_METASTASIS_DN, AP1_Q4_01, CHARAFE_BREAST_CANCER_BASAL_VS_MESENCHYMAL_UP, HNF4_DR1_Q3, MODULE_99, GOCC_MITOCHONDRIAL_ENVELOPE

GO Biological Process (1): phosphocreatine biosynthetic process (GO:0046314)

GO Molecular Function (8): creatine kinase activity (GO:0004111), ATP binding (GO:0005524), nucleotide binding (GO:0000166), catalytic activity (GO:0003824), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), transferase activity, transferring phosphorus-containing groups (GO:0016772)

GO Cellular Component (3): mitochondrion (GO:0005739), mitochondrial inner membrane (GO:0005743), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Metabolism of amino acids and derivatives	1
Metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
phosphocreatine metabolic process	1
phosphagen biosynthetic process	1
kinase activity	1
phosphotransferase activity, nitrogenous group as acceptor	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
molecular_function	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
transferase activity	1
cytoplasm	1
intracellular membrane-bounded organelle	1
organelle inner membrane	1
mitochondrial membrane	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1354 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CKMT1B	CATSPER2	Q96P56	948
CKMT1B	STRC	Q7RTU9	943
CKMT1B	SLC6A8	P48029	917
CKMT1B	PPIP5K1	Q6PFW1	867
CKMT1B	NME4	O00746	840
CKMT1B	GATM	P50440	800
CKMT1B	LDHAL6A	Q6ZMR3	734
CKMT1B	LDHAL6B	Q9BYZ2	732
CKMT1B	LDHC	P07864	707
CKMT1B	ASB9	Q96DX5	678
CKMT1B	GOT1L1	Q8NHS2	619
CKMT1B	GAMT	Q14353	604
CKMT1B	VDAC1	P21796	571
CKMT1B	LDHA	P00338	538
CKMT1B	GOT1	P17174	527

IntAct

127 interactions, top by confidence:

A	B	Type	Score
ASB9	CKM	psi-mi:“MI:0914”(association)	0.870
CKMT1A	ASB9	psi-mi:“MI:0915”(physical association)	0.740
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
CFTR	HAX1	psi-mi:“MI:0914”(association)	0.610
OCM	CKMT1A	psi-mi:“MI:0915”(physical association)	0.600
HPCA	CKMT1A	psi-mi:“MI:0915”(physical association)	0.560
CTNNA3	CKMT1A	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	NUTF2	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	RXRG	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	HPCA	psi-mi:“MI:0915”(physical association)	0.560
CKM	CKMT1A	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	PPP1R16A	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	PSMC3	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	CTNNA3	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	WFS1	psi-mi:“MI:0915”(physical association)	0.560
CKMT1A	JPH3	psi-mi:“MI:0915”(physical association)	0.560
ASB9	ARIH2	psi-mi:“MI:0914”(association)	0.530
CKMT1A	CKMT2	psi-mi:“MI:0915”(physical association)	0.500
CKMT2	CKMT1A	psi-mi:“MI:0914”(association)	0.500
	CAND2	psi-mi:“MI:0914”(association)	0.460
HTRA2	HAX1	psi-mi:“MI:2364”(proximity)	0.420

BioGRID (206): CKMT1A (Affinity Capture-MS), CKMT1B (Affinity Capture-MS), CKMT1A (Affinity Capture-MS), CKMT1A (Affinity Capture-MS), CKMT1B (Co-fractionation), CKMT1A (Co-fractionation), CKMT1B (Co-fractionation), CKMT1A (Co-fractionation), CKMT1B (Co-fractionation), CKMT1A (Co-fractionation), CKMT1B (Co-fractionation), CKMT1A (Co-fractionation), CKMT1B (Co-fractionation), CKMT1A (Co-fractionation), CKMT1B (Co-fractionation)

ESM2 similar proteins: A0A286R7K5, A0A976YI25, B0FRF9, B1PVZ9, C7E3T4, C9EIP1, H6VGI2, H6VGI3, O61367, O77814, O96507, P00563, P00564, P00565, P00566, P04414, P05123, P05124, P06732, P07310, P07335, P09605, P11009, P12532, P14208, P17540, P24722, P25809, P30275, P48610, P51541, P51545, P70079, P91798, Q004B5, Q04447, Q29577, Q29594, Q3ZBP1, Q5EA61

Diamond homologs: A0A286R7K5, A0A976YI25, A4J0X5, A5D5K7, A8F953, B0FRF9, B1PVZ9, C1KYG4, C7E3T4, C9EIP1, G1ESZ9, H6VGI2, H6VGI3, O15989, O15990, O15991, O15992, O61367, O77814, O96507, P00563, P00564, P00565, P00566, P00567, P04414, P05122, P05123, P05124, P06732, P07310, P07335, P09605, P11009, P12277, P12532, P14208, P16641, P17540, P18294

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
creatine	“up-regulates activity”	CKMT1A	“chemical activation”
CKMT1A	“up-regulates quantity”	N-phosphocreatine	“chemical modification”
ABL1	“up-regulates quantity by stabilization”	CKMT1A	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 114 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
SRP-dependent cotranslational protein targeting to membrane	7	8.7×	8e-03

GO biological processes:

GO term	Partners	Fold	FDR
cytoplasmic translation	6	10.5×	7e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	0
Uncertain significance	22
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (5)

Variant ID	HGVS	Classification
1526447	GRCh37/hg19 15q15.2-21.2(chr15:42850434-49592633)	Pathogenic
1879316	GRCh37/hg19 15q15.3(chr15:43888606-43941032)x0	Pathogenic
3024591	GRCh37/hg19 15q15.3(chr15:43873425-43941042)x1	Pathogenic
598749	Single allele	Pathogenic
625830	GRCh37/hg19 15q15.3(chr15:43890409-43939642)	Pathogenic

SpliceAI

3107 predictions. Top by Δscore:

Variant	Effect	Δscore
15:43595362:A:AG	acceptor_gain	1.0000
15:43595363:A:G	acceptor_gain	1.0000
15:43595369:CTTA:C	acceptor_loss	1.0000
15:43595370:TTAGG:T	acceptor_loss	1.0000
15:43595371:TAGGT:T	acceptor_loss	1.0000
15:43595372:A:AG	acceptor_gain	1.0000
15:43595372:AG:A	acceptor_gain	1.0000
15:43595373:G:A	acceptor_gain	1.0000
15:43595373:G:GA	acceptor_gain	1.0000
15:43595373:GGT:G	acceptor_gain	1.0000
15:43595373:GGTA:G	acceptor_gain	1.0000
15:43595373:GGTAT:G	acceptor_gain	1.0000
15:43595465:G:GG	donor_gain	1.0000
15:43595465:GTAAA:G	donor_loss	1.0000
15:43595466:TAAA:T	donor_gain	1.0000
15:43595467:AAA:A	donor_gain	1.0000
15:43595467:AAAG:A	donor_loss	1.0000
15:43595470:G:GG	donor_gain	1.0000
15:43595470:GT:G	donor_loss	1.0000
15:43596078:G:GG	donor_gain	1.0000
15:43596083:GGCCT:G	donor_gain	1.0000
15:43596205:A:AG	acceptor_gain	1.0000
15:43596205:A:AT	acceptor_loss	1.0000
15:43596206:G:A	acceptor_loss	1.0000
15:43596206:G:GG	acceptor_gain	1.0000
15:43596289:TTTGG:T	donor_loss	1.0000
15:43596290:TTGG:T	donor_loss	1.0000
15:43596291:TGGTA:T	donor_loss	1.0000
15:43596292:GGTAT:G	donor_loss	1.0000
15:43596294:T:A	donor_loss	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000758407 (15:43598631 C>G,T), RS1004284885 (15:43597752 A>G,T), RS1004320639 (15:43597617 T>G), RS1005292373 (15:43593056 T>G), RS1005326355 (15:43591346 G>A,C), RS1008049404 (15:43598524 C>G), RS1008085347 (15:43598109 T>C,G), RS1010397763 (15:43597098 T>A,C), RS1014291476 (15:43597565 T>A,C), RS1016413192 (15:43591401 G>A,T), RS1018464874 (15:43593079 C>T), RS1020515479 (15:43596583 A>C), RS1020752910 (15:43598533 C>T), RS1024322064 (15:43597570 T>A,C), RS1025391100 (15:43590989 G>A,T)

Disease associations

OMIM: gene MIM:123290 | disease phenotypes: MIM:611102, MIM:603720

GenCC curated gene-disease

Mondo (2): deafness-infertility syndrome (MONDO:0012621), autosomal recessive nonsyndromic hearing loss 16 (MONDO:0011364)

Orphanet (2): Deafness-infertility syndrome (Orphanet:94064), Rare autosomal recessive non-syndromic sensorineural deafness type DFNB (Orphanet:90636)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
C566339	Deafness, Autosomal Recessive 16 (supp.)
C567010	Deafness, Sensorineural, And Male Infertility (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6066961 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.00	Kd	9.912	nM	CHEMBL5653589
7.76	ED50	17.2	nM	CHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 2 total; 1 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
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148076: Binding affinity to human CKMT1A incubated for 45 mins by Kinobead based pull down assay	kd	0.0099	uM

CTD chemical–gene interactions

19 total (human), top 19 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	2
3,19-(2-bromobenzylidene)andrographolide	decreases expression, decreases response to substance	1
decabromobiphenyl ether	increases expression	1
afimoxifene	decreases response to substance	1
CGP 52608	affects binding, increases reaction	1
ICG 001	increases expression	1
abrine	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Atrazine	decreases expression	1
Benzo(a)pyrene	decreases methylation	1
Cisplatin	affects response to substance	1
Estradiol	affects cotreatment, decreases expression	1
Etoposide	affects response to substance	1
Methotrexate	affects response to substance	1
Tobacco Smoke Pollution	decreases expression	1
Mitomycin	affects response to substance	1
Cadmium Chloride	increases expression	1
Acrylamide	decreases expression	1
Particulate Matter	decreases expression, increases abundance	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5651118	Binding	Binding affinity to human CKMT1A incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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