MCTS1

Summary

MCTS1 (MCTS1 re-initiation and release factor, HGNC:23357) is a protein-coding gene on chromosome Xq24, encoding Malignant T-cell-amplified sequence 1 (Q9ULC4). Translation regulator forming a complex with DENR to promote translation reinitiation.

Enables RNA cap binding activity; ribosomal small subunit binding activity; and translation factor activity, non-nucleic acid binding. Involved in IRES-dependent viral translational initiation; cytoplasmic translational initiation; and ribosome disassembly. Is active in cytoplasm. Implicated in immunodeficiency 118.

Source: NCBI Gene 28985 — RefSeq curated summary.

At a glance

• Gene–disease (curated): immunodeficiency 118 (Strong, GenCC)
• Clinical variants (ClinVar): 59 total — 3 pathogenic
• Phenotypes (HPO): 12
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_014060

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23357
Approved symbol	MCTS1
Name	MCTS1 re-initiation and release factor
Location	Xq24
Locus type	gene with protein product
Status	Approved
Aliases	MCT-1
Ensembl gene	ENSG00000232119
Ensembl biotype	protein_coding
OMIM	300587
Entrez	28985

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 9 protein_coding, 4 protein_coding_CDS_not_defined

ENST00000371315, ENST00000371317, ENST00000484481, ENST00000487133, ENST00000493274, ENST00000493879, ENST00000859686, ENST00000938115, ENST00000938116, ENST00000938117, ENST00000938118, ENST00000938119, ENST00000938120

RefSeq mRNA: 2 — MANE Select: NM_014060 NM_001137554, NM_014060

CCDS: CCDS14601, CCDS48160

Canonical transcript exons

ENST00000371317 — 6 exons

Exon	Start	End
ENSE00001454933	120604101	120604247
ENSE00001741867	120612183	120621159
ENSE00003473073	120608225	120608358
ENSE00003547498	120605407	120605559
ENSE00003555415	120611011	120611078
ENSE00003589129	120606079	120606176

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 95.42.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 60.8194 / max 650.6485, expressed in 1820 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter ID	TPM avg	Samples expressed
197432	48.7653	1818
197430	3.4090	1581
197431	2.8187	1417
197429	2.5566	1425
197434	2.5283	992
197433	0.5220	229
197436	0.1188	29
197435	0.1009	36

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cortical plate	UBERON:0005343	95.42	gold quality
mucosa of transverse colon	UBERON:0004991	95.05	gold quality
islet of Langerhans	UBERON:0000006	93.76	gold quality
body of pancreas	UBERON:0001150	93.76	gold quality
prefrontal cortex	UBERON:0000451	93.61	gold quality
ganglionic eminence	UBERON:0004023	93.49	gold quality
pancreas	UBERON:0001264	93.30	gold quality
stromal cell of endometrium	CL:0002255	93.05	gold quality
endometrium	UBERON:0001295	92.98	gold quality
pituitary gland	UBERON:0000007	92.80	gold quality
adenohypophysis	UBERON:0002196	92.67	gold quality
tonsil	UBERON:0002372	92.53	gold quality
right adrenal gland	UBERON:0001233	92.50	gold quality
superior frontal gyrus	UBERON:0002661	92.37	gold quality
esophagus mucosa	UBERON:0002469	92.24	gold quality
rectum	UBERON:0001052	92.18	gold quality
frontal cortex	UBERON:0001870	92.16	gold quality
lower esophagus mucosa	UBERON:0035834	92.09	gold quality
left adrenal gland	UBERON:0001234	92.05	gold quality
left adrenal gland cortex	UBERON:0035825	91.85	gold quality
adrenal gland	UBERON:0002369	91.76	gold quality
right adrenal gland cortex	UBERON:0035827	91.74	gold quality
cerebral cortex	UBERON:0000956	91.62	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	91.47	gold quality
bone marrow cell	CL:0002092	91.33	gold quality
lymph node	UBERON:0000029	91.33	gold quality
right lobe of liver	UBERON:0001114	91.30	gold quality
cortex of kidney	UBERON:0001225	91.28	gold quality
heart left ventricle	UBERON:0002084	91.27	gold quality
placenta	UBERON:0001987	91.24	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	12.05

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SP1

miRNA regulators (miRDB)

309 targeting MCTS1, 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-8485	100.00	77.57	4731
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3134	100.00	66.43	777
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-4682	100.00	68.89	1258
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4531	99.99	69.70	3181
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-548C-3P	99.99	74.01	7587
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-485-3P	99.98	70.68	1585
HSA-MIR-539-3P	99.98	70.74	1616
HSA-MIR-548N	99.98	71.94	4170

Literature-anchored findings (GeneRIF, showing 23)

• tumor cell lines overexpressing MCT-1 exhibited increased growth rates and displayed increased protection against apoptosis induced by serum starvation (PMID:12637315)
• demonstrated the presence of sequence-specific DNA-binding protein in nuclear extracts designated as LMBF; the 26-mer oligonucleotide containing the LMBF binding site is required for maximum transcriptional activity of the MCT-1 promoter (PMID:12938157)
• role of the MCT-1 in lymphomagenesis (PMID:18824261)
• Loss of p53 and MCT-1 overexpression synergistically promote chromosome instability and tumorigenicity. (PMID:19372582)
• Results describe the expression and purification of MCT-1 in insect cells using a baculovirus expression system. (PMID:20076993)
• The result suggest that co-expression of CD147 and MCT1/MCT4 is related to drug resistance during EOC metastasis and could be useful therapeutic targets to prevent the development of incurable, recurrent and drug resistance EOC. (PMID:20658178)
• The present study indicates possible involvement of a protein kinase (PK)C- and PKA-mediated pathway associated with expression of MCT1 and lactate transport in rhabdomyosarcoma cells. (PMID:20823576)
• The oppositions between MCT-1 and p53 are firstly confirmed at multistage processes that include transcription control, mRNA metabolism, and protein expression (PMID:21138557)
• MCT-1 is a new centrosomal-associated oncoprotein, and that it plays a novel role in the regulation of mitosis signifies its important function in the process of tumorigenesis. (PMID:22336915)
• Overexpression of MCT1 is associated with gliomas. (PMID:23258846)
• DENR binds to the P-site of the 40S ribosomal subunit and together with MCTS1 forms a tRNA binding surface and interferes with eIF1/eIF2/eIF3 binding, thus operating in post-termination ribosome recycling and translation re-initiation (PMID:28723557)
• findings elucidate how the DENR-MCT-1 dimer interacts with the ribosome and have functional implications for the mechanism of unconventional translation initiation and reinitiation. (PMID:28723557)
• Reinitiation complexes involving initiation factors eIF2D, MCT-1, and DENR controls the translation of a large fraction of mammalian cellular mRNAs. (PMID:28732596)
• PKC inhibitor sotrastaurin induced cell apoptosis and cell cycle arrest in DLBCL cells potentially through regulating the expression of MCT-1 (PMID:29534146)
• Present the crystal structure of MCTS1 bound to a fragment of DENR. Based on this structure, we identify and experimentally validate that DENR residues Glu42, Tyr43, and Tyr46 are important for MCTS1 binding and that MCTS1 residue Phe104 is important for tRNA binding. Mutation of these residues reveals that DENR-MCTS1 dimerization and tRNA binding are both necessary for DENR and MCTS1 to promote translation reinitiation. (PMID:29889857)
• findings elucidate further the mechanism of regulation of DENR-MCT-1 activities in unconventional translation initiation, reinitiation, and recycling. (PMID:30584092)
• High MCT-1 expression is associated with M2-like polarization and triple-negative breast cancer cell invasion. (PMID:30885232)
• These results suggest MCT-1/miR-34a/IL-6/IL-6R axis is responsible for MCT-1-mediated effects on non-small cell lung cance cell stemness. (PMID:31891569)
• MCT1 expression is independently related to shorter cancer-specific survival in clear cell renal cell carcinoma. (PMID:34668521)
• Prognostic value of malignant T cell-amplified sequence 1 in head and neck squamous cell carcinoma. (PMID:34704820)
• MCTS1 promotes laryngeal squamous cell carcinoma cell growth via enhancing LARP7 stability. (PMID:35274760)
• MCTS1 enhances the proliferation of laryngeal squamous cell carcinoma via promoting OTUD6B-1 mediated LIN28B deubiquitination. (PMID:37634410)
• Human MCTS1-dependent translation of JAK2 is essential for IFN-gamma immunity to mycobacteria. (PMID:37875108)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	mcts1	ENSDARG00000025972
mus_musculus	Mcts1	ENSMUSG00000000355
rattus_norvegicus	Mcts1	ENSRNOG00000002563
drosophila_melanogaster	MCTS1	FBGN0029833
caenorhabditis_elegans		WBGENE00015703

Paralogs (1): MCTS2 (ENSG00000101898)

Protein

Protein identifiers

Malignant T-cell-amplified sequence 1 — Q9ULC4 (reviewed: Q9ULC4)

Alternative names: Multiple copies T-cell malignancies

All UniProt accessions (1): Q9ULC4

UniProt curated annotations — full annotation on UniProt →

Function. Translation regulator forming a complex with DENR to promote translation reinitiation. Translation reinitiation is the process where the small ribosomal subunit remains attached to the mRNA following termination of translation of a regulatory upstream ORF (uORF), and resume scanning on the same mRNA molecule to initiate translation of a downstream ORF, usually the main ORF (mORF). The MCTS1/DENR complex is pivotal to two linked mechanisms essential for translation reinitiation. Firstly, the dissociation of deacylated tRNAs from post-termination 40S ribosomal complexes during ribosome recycling. Secondly, the recruitment in an EIF2-independent manner of aminoacylated initiator tRNA to P site of 40S ribosomes for a new round of translation. This regulatory mechanism governs the translation of more than 150 genes which translation reinitiation is MCTS1/DENR complex-dependent. Consequently, modulates various unrelated biological processes including cell cycle regulation and DNA damage signaling and repair. Notably, it positively regulates interferon gamma immunity to mycobacteria by enhancing the translation of JAK2.

Subunit / interactions. Interacts (via PUA domain) with DENR; the complex regulates translation reinitiation.

Subcellular location. Cytoplasm.

Tissue specificity. Ubiquitous. Over-expressed in T-cell lymphoid cell lines and in non-Hodgkin lymphoma cell lines as well as in a subset of primary large B-cell lymphomas.

Post-translational modifications. Phosphorylation is critical for stabilization and promotion of cell proliferation.

Disease relevance. Immunodeficiency 118 (IMD118) [MIM:301115] An X-linked recessive disorder characterized by increased susceptibility to disseminated mycobacterial infections in infancy, notably after Bacillus Calmette-Guerin (BCG) vaccination. Initial clinical features include fever, lymphadenopathy, hepatosplenomegaly, abscesses, and osteomyelitis. Affected males usually recover with treatment, have no other infections, and show normal growth and development. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The PUA RNA-binding domain is critical for cap binding, but not sufficient for translation enhancer function. MCT1 N-terminal region is required to enhance translation possibly through interaction with other proteins.

Induction. By DNA damaging agents such as gamma irradiation, adriamycin or taxol in lymphoid cells, but not by stress stimuli such as heat shock. This induction of protein expression does not occur at the RNA level, and does not require new protein synthesis.

Similarity. Belongs to the MCTS1 family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q9ULC4-1	1	yes
Q9ULC4-2	2
Q9ULC4-3	3

RefSeq proteins (2): NP_001131026, NP_054779* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002478	PUA	Domain
IPR004521	Uncharacterised_CHP00451	Domain
IPR015947	PUA-like_sf	Homologous_superfamily
IPR016437	MCT-1/Tma20	Family
IPR041366	Pre-PUA	Domain

Pfam: PF01472, PF17832

UniProt features (33 total): helix 12, strand 10, modified residue 2, splice variant 2, mutagenesis site 2, chain 1, domain 1, turn 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
3R90	X-RAY DIFFRACTION	1.7
6MS4	X-RAY DIFFRACTION	2
5ONS	X-RAY DIFFRACTION	2.14
5VYC	X-RAY DIFFRACTION	6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9ULC4-F1	97.28	0.99

Functional residue map

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

Post-translational modifications (2): 81, 118

Mutagenesis-validated functional residues (2):

Position	Phenotype
81	no phosphorylation by mapk1; decreased stability of mcts1 protein; significant cell growth reduction.
118	no phosphorylation by cdk1; no cell growth alteration.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 238 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, MODULE_255, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, CHIANG_LIVER_CANCER_SUBCLASS_UNANNOTATED_DN, MODULE_317, GOBP_TRANSLATIONAL_INITIATION, GOMF_TRANSLATION_INITIATION_FACTOR_ACTIVITY, GGGTGGRR_PAX4_03, GGCNKCCATNK_UNKNOWN, GOBP_TRANSLATION, GATA3_01, GOBP_FORMATION_OF_TRANSLATION_PREINITIATION_COMPLEX, GOBP_CYTOPLASMIC_TRANSLATIONAL_INITIATION, MODULE_480, HFH8_01

GO Biological Process (7): formation of translation preinitiation complex (GO:0001731), translation reinitiation (GO:0002188), DNA damage response (GO:0006974), ribosome disassembly (GO:0032790), IRES-dependent viral translational initiation (GO:0075522), translation (GO:0006412), translational initiation (GO:0006413)

GO Molecular Function (5): RNA cap binding (GO:0000339), translation initiation factor activity (GO:0003743), ribosomal small subunit binding (GO:0043024), RNA binding (GO:0003723), protein binding (GO:0005515)

GO Cellular Component (1): cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cytoplasmic translational initiation	2
translational initiation	2
protein-RNA complex assembly	1
cellular response to stress	1
organelle disassembly	1
viral process	1
viral translation	1
peptidyltransferase activity	1
translational elongation	1
translational termination	1
macromolecule biosynthetic process	1
protein metabolic process	1
protein biosynthetic process	1
formation of translation initiation ternary complex	1
translation	1
metabolic process	1
RNA binding	1
translation factor activity	1
ribosome binding	1
nucleic acid binding	1
binding	1
intracellular anatomical structure	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1188 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MCTS1	DENR	O43583	957
MCTS1	CUL4B	Q13620	834
MCTS1	UBE2A	P49459	649
MCTS1	EMB	Q6PCB8	639
MCTS1	SLC16A3	O15427	638
MCTS1	SLC16A7	O60669	597
MCTS1	SLC16A4	O15374	593
MCTS1	BSG	P35613	589
MCTS1	CCNH	P51946	550
MCTS1	EIF1	P41567	539
MCTS1	SLC16A8	O95907	526
MCTS1	SLC16A10	Q8TF71	522
MCTS1	SLC16A2	P36021	497
MCTS1	EIF2D	P41214	469
MCTS1	CDT1	Q9H211	428

IntAct

71 interactions, top by confidence:

A	B	Type	Score
DENR	MCTS1	psi-mi:“MI:0915”(physical association)	0.870
MCTS1	DENR	psi-mi:“MI:0914”(association)	0.870
CTPS2	CTPS1	psi-mi:“MI:0914”(association)	0.850
FAM90A1	KPNA3	psi-mi:“MI:0914”(association)	0.670
GPX7	GAK	psi-mi:“MI:0914”(association)	0.640
SS18L2	SMARCA2	psi-mi:“MI:0914”(association)	0.570
CYP1A1	SNX3	psi-mi:“MI:0914”(association)	0.530
WASHC3	WASH3P	psi-mi:“MI:0914”(association)	0.530
JUN	TPM3	psi-mi:“MI:0914”(association)	0.350
Xpo1	IFT56	psi-mi:“MI:0914”(association)	0.350
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
ARHGAP35	CSTB	psi-mi:“MI:0914”(association)	0.350
ARHGAP11B	RPN1	psi-mi:“MI:0914”(association)	0.350
ARHGAP26	NUDT21	psi-mi:“MI:0914”(association)	0.350
HTRA4	PSMD12	psi-mi:“MI:0914”(association)	0.350
PAK4	MCM5	psi-mi:“MI:0914”(association)	0.350
rep	TMEM120B	psi-mi:“MI:0914”(association)	0.350
JAZF1	TNPO2	psi-mi:“MI:0914”(association)	0.350
	KIF5C	psi-mi:“MI:0914”(association)	0.350
	BANF1	psi-mi:“MI:0914”(association)	0.350
SUZ12	TNPO2	psi-mi:“MI:0914”(association)	0.350
MAPT	SHTN1	psi-mi:“MI:0914”(association)	0.350
GTF2E2	STX7	psi-mi:“MI:0914”(association)	0.350
PAGE1	CIBAR1	psi-mi:“MI:0914”(association)	0.350
FGB	KIF2A	psi-mi:“MI:0914”(association)	0.350
HOXC5	PDLIM1	psi-mi:“MI:0914”(association)	0.350

BioGRID (150): MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), CORO1C (Co-fractionation), DENR (Co-fractionation), MCTS1 (Co-fractionation), MCTS1 (Proximity Label-MS), MCTS1 (Proximity Label-MS), DENR (Two-hybrid), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS), MCTS1 (Affinity Capture-MS)

ESM2 similar proteins: A0A3B3IRV3, A0SXL6, A5DK38, A5PKR8, B6K286, O13914, O14179, P05197, P09445, P13188, P13639, P14325, P29691, P55823, P58252, P87313, P89886, Q07803, Q07953, Q09191, Q23716, Q25566, Q2KIE4, Q3SYU2, Q4G009, Q54Y20, Q554D9, Q5PPY1, Q5R8Z3, Q5ZI42, Q6BIJ0, Q6BPD3, Q6CA26, Q6CJ62, Q6DER1, Q6NRJ7, Q6P3J5, Q75AA8, Q75CZ5, Q7ZV34

Diamond homologs: A0A3B3IRV3, P87313, P89886, Q2KIE4, Q4G009, Q58827, Q5PPY1, Q5ZI42, Q6DER1, Q6NRJ7, Q75AA8, Q7ZV34, Q86KL4, Q9CQ21, Q9DB27, Q9ULC4, Q9W445, P0CL18, P41214, Q5RA63, B6YUR8, O57712, Q57878, Q5JHC0, Q8TH90, Q58CR3

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
MCTS1	“up-regulates activity”	DENR	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	3
Likely pathogenic	0
Uncertain significance	5
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (3)

Variant ID	HGVS	Classification
2691737	NM_014060.3(MCTS1):c.228dup (p.Pro77fs)	Pathogenic
2691738	NM_014060.3(MCTS1):c.213dup (p.Arg72Ter)	Pathogenic
2691739	NM_014060.3(MCTS1):c.164+3_164+6del	Pathogenic

SpliceAI

811 predictions. Top by Δscore:

Variant	Effect	Δscore
X:120604245:GAA:G	donor_gain	1.0000
X:120604248:G:GG	donor_gain	1.0000
X:120605388:T:A	acceptor_gain	1.0000
X:120605391:A:AG	acceptor_gain	1.0000
X:120605392:A:G	acceptor_gain	1.0000
X:120605394:A:AG	acceptor_gain	1.0000
X:120605398:ACTT:A	acceptor_gain	1.0000
X:120605556:GATG:G	donor_gain	1.0000
X:120605558:TGG:T	donor_loss	1.0000
X:120605560:G:A	donor_loss	1.0000
X:120605560:G:GG	donor_gain	1.0000
X:120605561:T:A	donor_loss	1.0000
X:120606177:G:GG	donor_gain	1.0000
X:120608223:A:AG	acceptor_gain	1.0000
X:120608224:G:GG	acceptor_gain	1.0000
X:120608306:GCT:G	donor_gain	1.0000
X:120608321:GAGC:G	donor_gain	1.0000
X:120608324:C:G	donor_gain	1.0000
X:120608344:G:GG	donor_gain	1.0000
X:120608372:GC:G	donor_gain	1.0000
X:120609668:G:GT	donor_gain	1.0000
X:120611074:GACAT:G	donor_gain	1.0000
X:120611077:ATG:A	donor_loss	1.0000
X:120611078:TGT:T	donor_loss	1.0000
X:120611079:G:GG	donor_gain	1.0000
X:120611079:GTAAG:G	donor_loss	1.0000
X:120611080:T:G	donor_loss	1.0000
X:120612181:A:AG	acceptor_gain	1.0000
X:120612182:G:GA	acceptor_gain	1.0000
X:120612182:GT:G	acceptor_gain	1.0000

AlphaMissense

1204 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:120605447:A:G	K18E	1.000
X:120605448:A:T	K18I	1.000
X:120608255:A:T	D98V	1.000
X:120608261:G:A	G100E	1.000
X:120608272:T:C	F104L	1.000
X:120608274:T:A	F104L	1.000
X:120608274:T:G	F104L	1.000
X:120608285:G:A	G108E	1.000
X:120608297:T:C	M112T	1.000
X:120608298:G:A	M112I	1.000
X:120608298:G:C	M112I	1.000
X:120608298:G:T	M112I	1.000
X:120608305:G:C	G115R	1.000
X:120608306:G:A	G115D	1.000
X:120611051:G:A	G146E	1.000
X:120605449:A:C	K18N	0.999
X:120605449:A:T	K18N	0.999
X:120605553:T:A	V53D	0.999
X:120605558:T:C	C55R	0.999
X:120608254:G:C	D98H	0.999
X:120608255:A:C	D98A	0.999
X:120608256:T:A	D98E	0.999
X:120608256:T:G	D98E	0.999
X:120608260:G:A	G100R	0.999
X:120608260:G:C	G100R	0.999
X:120608264:C:A	A101D	0.999
X:120608267:T:A	I102N	0.999
X:120608272:T:A	F104I	0.999
X:120608276:T:A	V105E	0.999
X:120608279:T:C	L106P	0.999

dbSNP variants (sampled 300 via entrez): RS1000389153 (X:120615375 A>G), RS1000502669 (X:120616753 A>G), RS1001420793 (X:120603674 C>A,T), RS1001449454 (X:120602434 G>A), RS1001658808 (X:120612610 G>T), RS1001808127 (X:120605767 C>G), RS1002062744 (X:120609658 G>A), RS1002090173 (X:120621627 A>T), RS1002110786 (X:120611975 T>G), RS1002181928 (X:120619403 T>C,G), RS1002395722 (X:120610092 C>T), RS1003115843 (X:120603451 G>A), RS1003915661 (X:120620499 T>G), RS1003961312 (X:120605258 G>A,T), RS1004140538 (X:120607064 C>T)

Disease associations

OMIM: gene MIM:300587 | disease phenotypes: MIM:301115

GenCC curated gene-disease

Disease	Classification	Inheritance
immunodeficiency 118	Strong	X-linked

Mondo (1): immunodeficiency 118 (MONDO:0958030)

Orphanet (0):

HPO phenotypes

12 total (12 of 12 shown, HPO-id order):

HPO	Term
HP:0001263	Global developmental delay
HP:0001419	X-linked recessive inheritance
HP:0001744	Splenomegaly
HP:0001954	Recurrent fever
HP:0002240	Hepatomegaly
HP:0002716	Lymphadenopathy
HP:0002754	Osteomyelitis
HP:0003593	Infantile onset
HP:0004313	Decreased circulating immunoglobulin concentration
HP:0011463	Childhood onset
HP:0020086	BCGitis
HP:0020087	BCGosis

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5724622 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (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
CHEMBL1232461	MOLIBRESIB	2	1,538

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

Binding affinities (BindingDB)

118 measured of 133 human assays (133 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3-cyclopropyl-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[3-(hydroxymethyl)phenyl]-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	1 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[6-(1-hydroxyethyl)-2-pyridinyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	1 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[3-fluoro-5-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	25 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-3-methyl-1-(2-methylpropyl)-5-[5-(2,2,2-trifluoro-1-hydroxyethyl)-3-pyridinyl]thieno[2,3-d]pyrimidine-2,4-dione	EC50	34 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-fluoro-5-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	40 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[3-(1-hydroxyethyl)phenyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	50 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-5-[3-(2,2,2-trifluoro-1-hydroxyethyl)phenyl]pyrrolo[3,4-d]pyridazin-4-one	EC50	50 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
2-[[1-[(2-Chlorophenyl)methyl]-5-[3- (cyclopropylmethoxy)phenyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid. 1HNMR (CDCl3): δ 0.25-0.29 (m, 2H), 0.58-0.63 (m, 2H), 14.16-1.20 (m, 1H), 1.55 (s, 6H), 5.58 (d, 2H), 4.63 (s, 2H), 5.42 (s, 2H), 6.40 (s, 1H), 6.374-6.78 (m, 2H), 6.84-6.93 (m, 2H), 7.18-7.28 (m, 3H), 7.33-7.35 (m, 1H).	IC50	54.5 nM	US-10202350: MCT4 inhibitors for treating disease
3-cyclopropyl-5-[2,4-difluoro-5-(hydroxymethyl)phenyl]-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	70 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[5-(1-hydroxyethyl)thiophen-3-yl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	70 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[5-(hydroxymethyl)-3-pyridinyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	75 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2,4-difluoro-3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	80 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-fluoro-3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	80 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-fluoro-5-(1-hydroxyethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	80 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[2-(hydroxymethyl)-4-pyridinyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	90 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-(hydroxymethyl)-1,3-thiazol-4-yl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	90 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-5-[5-(2,2,2-trifluoro-1-hydroxyethyl)thiophen-2-yl]pyrrolo[3,4-d]pyridazin-4-one	EC50	90 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
1-[[5-(4-Chlorophenyl)-1-[(2- chlorophenyl)methyl]pyrazol-3- yl]methoxy]cyclopropanecarboxylic acid 1H NMR (CD3OD, 400 MHz) δ 1.18- 1.32 (m, 3H), 1.64-1.80 (m, 1H), 4.61 (s, 2H), 5.42 (s, 2H), 6.52 (s, 1H), 6.60-6.80 (m, 1H), 7.20-52 (m, 7H).	IC50	100 nM	US-10202350: MCT4 inhibitors for treating disease
1-[[1-[(2-Chlorophenyl)methyl]-5-(3- methoxyphenyl)pyrazol-3- yl]methoxy]cyclobutanecarboxylic acid. 1HNMR (CDCl3): δ 1.78-1.85 (m 1H), 1.95-2.04 (m, 2H), 2.18-2.25 (m, 1H), 3.09-3.14 (m, 1H), 3.66 (s, 3H), 4.27-4.32 (m, 1H), 4.55-4.65 (dd, 2H), 5.43 (s, 2H), 6.44 (s, 1H), 6.73-6.91 (m, 4H), 7.17-7.34 (m 4).	IC50	100 nM	US-10202350: MCT4 inhibitors for treating disease
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[2-fluoro-3-(hydroxymethyl)-5-methylphenyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	100 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
3-cyclopropyl-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[2-fluoro-3-(hydroxymethyl)-5-methylphenyl]-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	100 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	100 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[3-(1-hydroxyethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	100 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-5-[2-(2,2,2-trifluoro-1-hydroxyethyl)-1,3-thiazol-4-yl]pyrrolo[3,4-d]pyridazin-4-one	EC50	100 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[3,4-difluoro-5-(hydroxymethyl)phenyl]-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	160 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[6-fluoro-5-(hydroxymethyl)-3-pyridinyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	200 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[2-fluoro-5-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	200 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
2-[[1-[(2-Chlorophenyl)methyl]-5-[3- (cyclobutoxy)phenyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid. 1HNMR (CDCl3): δ 1.49-1.61 (m, 7H), m1.75-1.82 (m 1H), 2.01-2.11 (m 2H), 2.17-2.24 (m 2H), 4.37-4.45 (m 1H), 4.62 (s, 2H), 5.42 (s, 2H), 6.39 (s, 1H), 6.64 (s, 1H), 6.75-6.86 (m, 3H), 7.19-7.35 (m 4H).	IC50	204 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[1-[(2-Chlorophenyl)methyl]-5-[3- (cyclopentylmethoxy)phenyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid. 1HNMR (CDCl3): δ 1.25-1.29 (m, 2H), 1.55-1.61 (m, 10H), 1.76-1.79 (m, 2H), 2.24-2.31 (m, 1H), 3.59 (d, 2H), 4.62 (s, 2H), 5.43 (s, 2H), 6.41 (s, 1H), 6.73-6.91 (m, 4H), 7.19-7.35 (m, 4H).	IC50	204 nM	US-10202350: MCT4 inhibitors for treating disease
3-cyclopropyl-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[4-fluoro-3-(hydroxymethyl)phenyl]-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	220 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[5-(hydroxymethyl)-1,3-thiazol-2-yl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	300 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
2-[[1-[(2-Chlorophenyl)methyl]-5-(3- isobutoxyphenyl)pyrazol-3-yl]methoxy]-2- methyl-propanoic acid. 1HNMR (CDCl3): δ 0.95 (s, 3H)(, 0.96 (s, 3H), 1.56 (s, 6H), 1.97-2.03 (m, 1H), 3.49 (d, 2H), 4.63 (s, 2H), 5.43 (s, 2H), 6.41 (s, 1H), 6.73-6.80 (m, 2H), 6.84- 6.92 (m, 2H), 7.19-7.28 (m, 3H), 7.33- 7.35 (m, 1H).	IC50	302 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[5-(4-Chlorophenyl)-1-[(2,4- dichlorophenyl)methyl]pyrazol-3- yl]methoxy]acetic acid 1H NMR (DMSO-d6, 400 MHz) δ 3.80 (s, 2H), 4.50 9s, 2H), 5.30 (s, 2H), 6.50 (s, 1H), 6.60-80 (m, 1H), 7.20-70 (m, 6H).	IC50	303 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[1-[(2-chlorophenyl)methyl]-5-(3-methoxyphenyl)pyrazol-3-yl]methoxy]-2-methyl-N-methylsulfonylpropanamide	IC50	303 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[5-(4-Chlorophenyl)-1-[(2,4- dichlorophenyl)methyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid 1H NMR (CD3OD, 400 MHz) δ 1.48 (s, 6H), 4.58 (s, 2H), 5.40 (s, 2H), 6.54 (s, 1H), 6.73 (d, 1H), 7.20-7.38 (m, 3H), 7.40-48 (m, 3H).	IC50	400 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[5-(3-Chlorophenyl)-1-[(2- chlorophenyl)methyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid 1H NMR (CD3OD, 400 MHz) δ 1.32 (S, 6h) 4.58 (s, 2H), 5.42 (s, 2H), 6.57 (s, 1H), 6.67-6.80 (m, 1H), 7.22-7.30 (m, 3H), 7.32-42 (m, 4H).	IC50	404 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[1-[(2-Chlorophenyl)methyl]-5-[3- (cyclobutylmethoxy)phenyl]pyrazol-3- yl]methoxy]-2-methyl-propanoic acid. 1HNMR (CDCl3): δ 1.55 (s, 6H), 1.75- 1.82 (m, 2H), 1.85-1.98 (m, 2H), 2.06- 2.14 (m, 2H), 2.64-2.70 (m, 1H), 3.71 (d, 2H), 4.63 (s, 2H), 5.43 (s, 2H), 6.42 (s, 1H), 6.75-6.92 (m, 4H), 7.20-7.36 (m, 4).	IC50	404 nM	US-10202350: MCT4 inhibitors for treating disease
2-[[5-(4-Chlorophenyl)-1-[(2- chlorophenyl)methyl]pyrazol-3- yl]methoxy]-2-methyl-propanamide 1H NMR (CD3OD 400 MHz) δ 1.46 (s, 6H), 4.58 (s, 2H), 5.40 (s, 2H), 6.52 (s, 1H), 6.71-6.76 (m, 1H), 7.20-7.58 (m, 6H)	IC50	454 nM	US-10202350: MCT4 inhibitors for treating disease
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-chloro-5-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	600 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[2-fluoro-5-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-[(4-phenylphenyl)methyl]pyrrolo[3,4-d]pyridazin-4-one	EC50	800 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
3-cyclopropyl-5-[3,4-difluoro-5-(hydroxymethyl)phenyl]-6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione	EC50	900 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[5-(hydroxymethyl)-3-pyridinyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	900 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-3-methyl-1-(2-methylpropyl)-5-[2,4,6-trifluoro-3-(hydroxymethyl)phenyl]thieno[2,3-d]pyrimidine-2,4-dione	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
5-[3-(1-hydroxyethyl)phenyl]-3-methyl-1-(2-methylpropyl)-6-[(4-phenylphenyl)methyl]pyrrolo[3,4-d]pyridazin-4-one	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(2-chloroquinolin-4-yl)methyl]-5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[(1-chloroisoquinolin-4-yl)methyl]-5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[2-(2-chlorophenoxy)ethyl]-5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
6-[[2-(aminomethylamino)quinolin-4-yl]methyl]-5-[3-(hydroxymethyl)phenyl]-3-methyl-1-(2-methylpropyl)pyrrolo[3,4-d]pyridazin-4-one	EC50	5500 nM	US-10329303: Heterocyclic inhibitors of monocarboxylate transporter
2-[[1-[(2-chlorophenyl)methyl]-5-(3-propan-2-ylphenyl)pyrazol-3-yl]methoxy]-2-methylpropanoic acid	IC50	6000 nM	US-10202350: MCT4 inhibitors for treating disease

ChEMBL bioactivities

16 potent at pChembl≥5 of 77 total, top 16 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.26	IC50	54.5	nM	CHEMBL5981118
7.00	IC50	100	nM	CHEMBL5874865
7.00	IC50	100	nM	CHEMBL6018589
6.69	IC50	204	nM	CHEMBL5898165
6.69	IC50	204	nM	CHEMBL5904074
6.52	IC50	303	nM	CHEMBL6052282
6.52	IC50	302	nM	CHEMBL6031816
6.52	IC50	303	nM	CHEMBL5883085
6.40	IC50	400	nM	CHEMBL5918774
6.39	IC50	404	nM	CHEMBL5764687
6.39	IC50	404	nM	CHEMBL6017525
6.34	IC50	454	nM	CHEMBL5985401
5.22	IC50	6000	nM	CHEMBL6032683
5.05	IC50	9000	nM	CHEMBL5748717
5.00	IC50	1e+04	nM	MOLIBRESIB
5.00	IC50	1e+04	nM	CHEMBL5929597

PubChem BioAssay actives

1 with measured affinity, of 6 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
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2178799: Inhibition of MCTS1 (unknown origin) incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	ic50	10.0000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression	2
Air Pollutants	affects expression, increases abundance, decreases expression	2
aristolochic acid I	increases expression	1
bisphenol A	decreases expression	1
pyrogallol 1,3-dimethyl ether	affects localization, decreases expression, affects cotreatment	1
quercitrin	decreases expression	1
cobaltous chloride	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
beta-methylcholine	affects expression	1
epigallocatechin gallate	decreases expression, affects cotreatment	1
di-n-butylphosphoric acid	affects expression	1
Grape Seed Proanthocyanidins	affects cotreatment, decreases expression	1
jinfukang	decreases expression	1
bisphenol AF	increases expression	1
Sunitinib	decreases expression	1
Arsenic Trioxide	increases expression	1
Benzene	decreases expression	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Catechin	affects cotreatment, decreases expression	1
Dinitrochlorobenzene	decreases expression	1
Doxorubicin	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Eugenol	decreases expression	1
Furaldehyde	increases expression, affects cotreatment, affects localization	1
Hydrogen Peroxide	affects expression	1
Ivermectin	decreases expression	1
Methotrexate	increases expression	1
Oxazolone	decreases expression	1
Ozone	affects expression, increases abundance	1
Ribonucleotides	affects binding	1

ChEMBL screening assays

7 unique, capped per target: 7 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5697529	Binding	Inhibition of MCTS1 (unknown origin) assessed as fold change at 10 uM incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. — Nature

Cellosaurus cell lines

3 cell lines: 3 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_F0S0	NIH 3T3 MCT-1	Spontaneously immortalized cell line	Male
CVCL_F0S1	NIH 3T3 MCT-1-S118A	Spontaneously immortalized cell line	Male
CVCL_F0S2	NIH 3T3 MCT-1-T81A	Spontaneously immortalized cell line	Male

Clinical trials (associated diseases)

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