GTF3C4

Summary

GTF3C4 (general transcription factor IIIC subunit 4, HGNC:4667) is a protein-coding gene on chromosome 9q34.13, encoding General transcription factor 3C polypeptide 4 (Q9UKN8). Essential for RNA polymerase III to make a number of small nuclear and cytoplasmic RNAs, including 5S RNA, tRNA, and adenovirus-associated (VA) RNA of both cellular and viral origin. It is a selective cancer dependency (DepMap: 67.5% of cell lines).

Enables RNA polymerase III general transcription initiation factor activity and histone H3K14 acetyltransferase activity. Predicted to be involved in 5S class rRNA transcription by RNA polymerase III; tRNA transcription by RNA polymerase III; and transcription initiation at RNA polymerase III promoter. Located in mitochondrion and nucleoplasm. Part of transcription factor TFIIIC complex.

Source: NCBI Gene 9329 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 83 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 67.5% of screened cell lines
• MANE Select transcript: NM_012204

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4667
Approved symbol	GTF3C4
Name	general transcription factor IIIC subunit 4
Location	9q34.13
Locus type	gene with protein product
Status	Approved
Aliases	TFIIIC90, KAT12
Ensembl gene	ENSG00000125484
Ensembl biotype	protein_coding
OMIM	604892
Entrez	9329

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000372146, ENST00000483873, ENST00000898845

RefSeq mRNA: 1 — MANE Select: NM_012204 NM_012204

CCDS: CCDS6953

Canonical transcript exons

ENST00000372146 — 5 exons

Exon	Start	End
ENSE00000855989	132677977	132679803
ENSE00003296099	132683563	132683693
ENSE00003298522	132688881	132694953
ENSE00003378363	132687239	132687327
ENSE00003841303	132670464	132670955

Expression profiles

Bgee: expression breadth ubiquitous, 251 present calls, max score 85.94.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 9.1700 / max 50.1962, expressed in 1783 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
99165	4.7642	1616
99164	4.2113	1688
205641	0.1945	61

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
type B pancreatic cell	CL:0000169	85.94	gold quality
olfactory bulb	UBERON:0002264	85.53	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	85.29	gold quality
diaphragm	UBERON:0001103	85.18	gold quality
ventricular zone	UBERON:0003053	84.48	gold quality
gingival epithelium	UBERON:0001949	84.40	silver quality
islet of Langerhans	UBERON:0000006	84.14	gold quality
gingiva	UBERON:0001828	83.39	gold quality
ganglionic eminence	UBERON:0004023	82.90	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	82.77	gold quality
cortical plate	UBERON:0005343	82.65	gold quality
hair follicle	UBERON:0002073	81.98	silver quality
stromal cell of endometrium	CL:0002255	81.75	gold quality
squamous epithelium	UBERON:0006914	81.63	silver quality
esophagus squamous epithelium	UBERON:0006920	81.42	gold quality
middle temporal gyrus	UBERON:0002771	81.36	silver quality
upper leg skin	UBERON:0004262	81.30	gold quality
embryo	UBERON:0000922	81.19	gold quality
Brodmann (1909) area 23	UBERON:0013554	81.06	gold quality
male germ cell	CL:0000015	80.98	silver quality
tibia	UBERON:0000979	80.74	gold quality
parietal pleura	UBERON:0002400	80.59	gold quality
sperm	CL:0000019	80.35	gold quality
skin of hip	UBERON:0001554	80.18	gold quality
pleura	UBERON:0000977	79.53	gold quality
adrenal tissue	UBERON:0018303	79.29	gold quality
smooth muscle tissue	UBERON:0001135	79.27	gold quality
epithelium of esophagus	UBERON:0001976	79.22	gold quality
cartilage tissue	UBERON:0002418	79.00	gold quality
cerebellar vermis	UBERON:0004720	78.63	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	4.34

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

255 targeting GTF3C4, 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-3613-3P	100.00	76.36	7965
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-3925-3P	100.00	69.95	1237
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-4692	100.00	67.32	2066
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4514	99.99	67.10	1870
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 67.5% of screened cell lines.

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	gtf3c4	ENSDARG00000069538
mus_musculus	Gtf3c4	ENSMUSG00000035666
rattus_norvegicus	Gtf3c4	ENSRNOG00000054725

Protein

Protein identifiers

General transcription factor 3C polypeptide 4 — Q9UKN8 (reviewed: Q9UKN8)

Alternative names: TF3C-delta, Transcription factor IIIC 90 kDa subunit, Transcription factor IIIC subunit delta

All UniProt accessions (2): Q9UKN8, F2Z356

UniProt curated annotations — full annotation on UniProt →

Function. Essential for RNA polymerase III to make a number of small nuclear and cytoplasmic RNAs, including 5S RNA, tRNA, and adenovirus-associated (VA) RNA of both cellular and viral origin. Has histone acetyltransferase activity (HAT) with unique specificity for free and nucleosomal H3. May cooperate with GTF3C5 in facilitating the recruitment of TFIIIB and RNA polymerase through direct interactions with BRF1, POLR3C and POLR3F. May be localized close to the A box.

Subunit / interactions. Part of the TFIIIC subcomplex TFIIIC2, consisting of six subunits, GTF3C1, GTF3C2, GTF3C3, GTF3C4, GTF3C5 and GTF3C6. Interacts with BRF1, GTF3C1, GTF3C2, GTF3C5, GTF3C6, POLR3C and POLR3F.

Subcellular location. Nucleus.

Similarity. Belongs to the TFIIIC subunit 4 family.

RefSeq proteins (1): NP_036336* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR024761	TFIIIC_delta_N	Domain
IPR024764	TFIIIC_Znf	Domain
IPR036322	WD40_repeat_dom_sf	Homologous_superfamily
IPR044230	GTF3C4	Family
IPR045803	DUF5921	Domain

Pfam: PF12657, PF12660, PF19336

Enzyme classification (BRENDA):

• EC 2.3.1.48 — histone acetyltransferase (BRENDA: 41 organisms, 681 substrates, 1134 inhibitors, 140 Km, 96 kcat entries)

Substrate kinetics (BRENDA)

27 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ACETYL-COA	0.0002–0.046	51
HISTONE H3	0.007–2.09	23
HISTONE H4	—	11
HISTONE H4 PEPTIDE	0.0208–0.197	7
HISTONE	0.075–1.4	6
HISTONE H3 TAIL PEPTIDE	0.044–0.112	4
PICCOLONUA4 PEPTIDE	0.135–0.372	4
3-AZIDOPROPIONYL-COA	0.0002–0.0086	3
4-PENTYNOYL-COA	0.0009–0.0859	3
SPERMIDINE	0.18–0.27	3
5-HEXYNOYL-COA	0.0006–0.0117	2
6-HEPTYNOYL-COA	0.0003–0.0237	2
HISTONE H3-PEPTIDE	0.05–0.49	2
PROTEIN P53	1.28–4.63	2
3-AZIDOPROPANOYL-COA	0.0103	1

Catalyzed reactions (Rhea), 1 shown:

• L-lysyl-[protein] + acetyl-CoA = N(6)-acetyl-L-lysyl-[protein] + CoA + H(+) (RHEA:45948)

UniProt features (75 total): strand 36, helix 15, turn 8, sequence conflict 6, modified residue 5, region of interest 2, cross-link 2, chain 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
8CLI	ELECTRON MICROSCOPY	3.2
8CLJ	ELECTRON MICROSCOPY	3.2
8CLL	ELECTRON MICROSCOPY	3.4

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UKN8-F1	82.73	0.57

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 (7): 1, 19, 604, 611, 652, 225, 629

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

ID	Pathway
R-HSA-749476	RNA Polymerase III Abortive And Retractive Initiation
R-HSA-76061	RNA Polymerase III Transcription Initiation From Type 1 Promoter
R-HSA-76066	RNA Polymerase III Transcription Initiation From Type 2 Promoter
R-HSA-74158	RNA Polymerase III Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-76046	RNA Polymerase III Transcription Initiation

MSigDB gene sets: 176 (showing top): GOBP_TRNA_METABOLIC_PROCESS, GOBP_TRANSCRIPTION_BY_RNA_POLYMERASE_III, GGGTGGRR_PAX4_03, GOBP_RRNA_TRANSCRIPTION, EFC_Q6, WEI_MYCN_TARGETS_WITH_E_BOX, GOBP_DNA_TEMPLATED_TRANSCRIPTION_INITIATION, SANSOM_APC_TARGETS_UP, DODD_NASOPHARYNGEAL_CARCINOMA_UP, MODULE_48, GOBP_CHROMATIN_REMODELING, DANG_BOUND_BY_MYC, GRADE_COLON_AND_RECTAL_CANCER_DN, MODULE_95, BENPORATH_OCT4_TARGETS

GO Biological Process (5): transcription by RNA polymerase III (GO:0006383), transcription initiation at RNA polymerase III promoter (GO:0006384), 5S class rRNA transcription by RNA polymerase III (GO:0042791), tRNA transcription by RNA polymerase III (GO:0042797), chromatin remodeling (GO:0006338)

GO Molecular Function (8): RNA polymerase III general transcription initiation factor activity (GO:0000995), DNA binding (GO:0003677), histone H3K14 acetyltransferase activity (GO:0036408), histone acetyltransferase activity (GO:0004402), protein binding (GO:0005515), transferase activity (GO:0016740), acyltransferase activity (GO:0016746), protein-lysine-acetyltransferase activity (GO:0061733)

GO Cellular Component (4): transcription factor TFIIIC complex (GO:0000127), nucleoplasm (GO:0005654), mitochondrion (GO:0005739), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
RNA Polymerase III Transcription	2
RNA Polymerase III Transcription Initiation	2
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transcription by RNA polymerase III	4
intracellular membrane-bounded organelle	2
DNA-templated transcription	1
DNA-templated transcription initiation	1
rRNA transcription	1
tRNA transcription	1
chromatin organization	1
general transcription initiation factor activity	1
nucleic acid binding	1
histone H3 acetyltransferase activity	1
protein-lysine-acetyltransferase activity	1
histone modifying activity	1
binding	1
catalytic activity	1
transferase activity	1
protein N-acetyltransferase activity	1
RNA polymerase III transcription regulator complex	1
nuclear lumen	1
cellular anatomical structure	1
cytoplasm	1

Protein interactions and networks

STRING

1126 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GTF3C4	GTF3C5	Q9Y5Q8	987
GTF3C4	GTF3C1	Q12789	960
GTF3C4	GTF3C3	Q9Y5Q9	952
GTF3C4	GTF3C6	Q969F1	947
GTF3C4	BRF1	Q92994	860
GTF3C4	GTF3C2	Q8WUA4	822
GTF3C4	TAF1	P21675	555
GTF3C4	TCF7	P36402	545
GTF3C4	POLR3A	O14802	537
GTF3C4	ELP3	Q9H9T3	506
GTF3C4	HAUS4	Q9H6D7	464
GTF3C4	POLR3F	Q9H1D9	455
GTF3C4	BDP1	A6H8Y1	447
GTF3C4	C9orf40	Q8IXQ3	434
GTF3C4	NAA60	Q9H7X0	416

IntAct

103 interactions, top by confidence:

A	B	Type	Score
CDK8	MED19	psi-mi:“MI:2364”(proximity)	0.850
PLK1	SPAG9	psi-mi:“MI:0914”(association)	0.790
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
GTF3C1	GTF3C2	psi-mi:“MI:0914”(association)	0.670
PLK1	C1orf226	psi-mi:“MI:0914”(association)	0.560
ZNF764	IPO8	psi-mi:“MI:0914”(association)	0.530
ZNF764	SH3PXD2B	psi-mi:“MI:0914”(association)	0.530
GTF3C2	C1QBP	psi-mi:“MI:0914”(association)	0.530
FOXM1	PES1	psi-mi:“MI:0914”(association)	0.500
GTF3C6	GTF3C4	psi-mi:“MI:0915”(physical association)	0.500
FAIM	WDR47	psi-mi:“MI:0914”(association)	0.500
GTF3C3	GTF3C4	psi-mi:“MI:0915”(physical association)	0.500
DDX21	MED19	psi-mi:“MI:2364”(proximity)	0.480
ESR2	FBLL1	psi-mi:“MI:0914”(association)	0.460
H3C1	SMCHD1	psi-mi:“MI:2364”(proximity)	0.410
Gtf3c6		psi-mi:“MI:0915”(physical association)	0.400
Rpl35	RPS6	psi-mi:“MI:0914”(association)	0.350
Bag2		psi-mi:“MI:0914”(association)	0.350
NOP56	C12orf43	psi-mi:“MI:0914”(association)	0.350
Gtf3c2	PAPD5	psi-mi:“MI:0914”(association)	0.350
Gtf3c3	GTF3C1	psi-mi:“MI:0914”(association)	0.350
CBX8	CMSS1	psi-mi:“MI:0914”(association)	0.350
FOXB1	DDX39A	psi-mi:“MI:0914”(association)	0.350
FOXJ2	TCERG1	psi-mi:“MI:0914”(association)	0.350
FOXL1	DDX39A	psi-mi:“MI:0914”(association)	0.350
FOXQ1	DDX39A	psi-mi:“MI:0914”(association)	0.350
FOXS1	DDX39A	psi-mi:“MI:0914”(association)	0.350

BioGRID (255): GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-RNA), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS), GTF3C4 (Affinity Capture-MS)

ESM2 similar proteins: A0A1L8GXY4, A4D1P6, A8XSV3, B0JZ65, B0R160, B0WYR6, E9Q7R9, F1REV3, F6S215, O00443, O65418, P50748, Q09178, Q12769, Q17I16, Q19317, Q2TAW0, Q3MHH2, Q402B2, Q4V9P9, Q5R6T6, Q5RAY1, Q5RB52, Q5RE88, Q5ZJY3, Q5ZL79, Q5ZLL7, Q6DTM3, Q6GM71, Q6INI5, Q6P996, Q6X9E4, Q6ZQQ6, Q7TMQ7, Q86XI2, Q8BJW5, Q8BMQ2, Q8C3Y4, Q8K3E5, Q8N157

Diamond homologs: Q8BMQ2, Q9UKN8

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
GTF3C4	“form complex”	TFIIIC	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 138 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
S Phase	6	11.6×	4e-03
Orc1 removal from chromatin	5	9.5×	6e-03
Signaling by NOTCH	5	9.3×	6e-03
G2/M Checkpoints	6	8.6×	4e-03
Viral Infection Pathways	12	3.9×	4e-03
Infectious disease	13	3.4×	5e-03

GO biological processes:

GO term	Partners	Fold	FDR
transcription by RNA polymerase III	5	32.7×	2e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	69
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1013 predictions. Top by Δscore:

Variant	Effect	Δscore
9:132670951:TCAAA:T	donor_gain	1.0000
9:132670952:CAAA:C	donor_gain	1.0000
9:132670953:AAA:A	donor_gain	1.0000
9:132670953:AAAG:A	donor_loss	1.0000
9:132670954:AA:A	donor_gain	1.0000
9:132670954:AAGTA:A	donor_loss	1.0000
9:132670955:AG:A	donor_loss	1.0000
9:132670956:G:GG	donor_gain	1.0000
9:132670956:GTAA:G	donor_loss	1.0000
9:132677969:A:AG	acceptor_gain	1.0000
9:132677970:T:G	acceptor_gain	1.0000
9:132677972:TTCA:T	acceptor_loss	1.0000
9:132677973:TCA:T	acceptor_loss	1.0000
9:132677974:CAG:C	acceptor_loss	1.0000
9:132677975:A:AG	acceptor_gain	1.0000
9:132677975:AG:A	acceptor_gain	1.0000
9:132677975:AGGTT:A	acceptor_gain	1.0000
9:132677976:G:GC	acceptor_gain	1.0000
9:132677976:GG:G	acceptor_gain	1.0000
9:132677976:GGT:G	acceptor_gain	1.0000
9:132677976:GGTT:G	acceptor_gain	1.0000
9:132677976:GGTTG:G	acceptor_gain	1.0000
9:132683691:CCGG:C	donor_loss	1.0000
9:132683694:G:GG	donor_gain	1.0000
9:132683694:GTAAG:G	donor_loss	1.0000
9:132683695:T:A	donor_loss	1.0000
9:132687234:TTCA:T	acceptor_loss	1.0000
9:132687235:TCA:T	acceptor_loss	1.0000
9:132687236:CA:C	acceptor_loss	1.0000
9:132687237:A:AC	acceptor_loss	1.0000

AlphaMissense

5419 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:132678619:G:T	G334W	1.000
9:132678124:T:A	W169R	0.999
9:132678124:T:C	W169R	0.999
9:132678223:T:A	W202R	0.999
9:132678223:T:C	W202R	0.999
9:132678376:T:A	W253R	0.999
9:132678376:T:C	W253R	0.999
9:132678481:T:A	W288R	0.999
9:132678481:T:C	W288R	0.999
9:132678619:G:A	G334R	0.999
9:132678619:G:C	G334R	0.999
9:132678620:G:A	G334E	0.999
9:132678631:G:A	G338R	0.999
9:132678631:G:C	G338R	0.999
9:132678632:G:A	G338E	0.999
9:132678698:T:A	V360D	0.999
9:132678704:T:C	L362S	0.999
9:132678706:T:A	W363R	0.999
9:132678706:T:C	W363R	0.999
9:132678820:T:A	W401R	0.999
9:132678820:T:C	W401R	0.999
9:132678827:T:C	L403P	0.999
9:132678830:T:C	L404P	0.999
9:132678847:G:T	G410W	0.999
9:132678848:G:A	G410E	0.999
9:132678851:T:C	L411P	0.999
9:132678968:T:C	L450P	0.999
9:132679001:T:C	F461S	0.999
9:132679066:A:C	S483R	0.999
9:132679068:C:A	S483R	0.999

dbSNP variants (sampled 300 via entrez): RS1000216176 (9:132686131 T>C), RS1000751178 (9:132685937 C>G), RS1000778802 (9:132695087 A>C), RS1000831683 (9:132668422 C>A), RS1000938799 (9:132676111 GGATGGTCTC>G), RS1000996367 (9:132670494 G>A,T), RS1001047248 (9:132670602 A>G), RS1001130672 (9:132692317 A>G), RS1001373137 (9:132668653 C>T), RS1001621149 (9:132673178 G>A,C,T), RS1001662952 (9:132672636 G>A), RS1001715517 (9:132672974 G>A), RS1001846808 (9:132677346 G>A), RS1001846988 (9:132692693 A>G), RS1001914710 (9:132679612 A>G)

Disease associations

OMIM: gene MIM:604892 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5724603 (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)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 2.3.1.48 Histone acetyltransferases (HATs)

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
5.05	IC50	8960	nM	MOLIBRESIB

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	2178901: Inhibition of GTF3C4 (unknown origin) incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	ic50	8.9600	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Estradiol	increases expression	2
Tobacco Smoke Pollution	increases expression	2
Cadmium Chloride	decreases expression, increases expression	2
FR900359	affects phosphorylation	1
2,4,6-tribromophenol	decreases expression	1
triphenyl phosphate	affects expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
bisphenol A	decreases expression	1
decabromobiphenyl ether	decreases expression	1
2-butenal	decreases expression	1
cobaltous chloride	increases expression	1
tetrabromobisphenol A	decreases expression	1
potassium chromate(VI)	increases expression, affects cotreatment	1
coumarin	affects phosphorylation	1
epigallocatechin gallate	affects cotreatment, increases expression	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
Sunitinib	increases expression	1
Zoledronic Acid	increases expression	1
Arsenic	affects methylation	1
Benzo(a)pyrene	increases expression	1
Ivermectin	decreases expression	1
Methyl Methanesulfonate	decreases expression	1
Phenobarbital	affects expression	1
Plant Oils	increases expression	1

ChEMBL screening assays

6 unique, capped per target: 6 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5697631	Binding	Inhibition of GTF3C4 (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

Clinical trials (associated diseases)

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