ECPAS

Summary

ECPAS (Ecm29 proteasome adaptor and scaffold, HGNC:29020) is a protein-coding gene on chromosome 9q31.3, encoding Proteasome adapter and scaffold protein ECM29 (Q5VYK3). Adapter/scaffolding protein that binds to the 26S proteasome, motor proteins and other compartment specific proteins.

Enables proteasome binding activity. Involved in ERAD pathway. Located in several cellular components, including centrosome; cytoplasmic vesicle; and nucleoplasm.

Source: NCBI Gene 23392 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 368 total
• Druggable target: yes
• MANE Select transcript: NM_001364929

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:29020
Approved symbol	ECPAS
Name	Ecm29 proteasome adaptor and scaffold
Location	9q31.3
Locus type	gene with protein product
Status	Approved
Aliases	FLJ22036, ECM29
Ensembl gene	ENSG00000136813
Ensembl biotype	protein_coding
OMIM	616694
Entrez	23392

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 14 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000259335, ENST00000338205, ENST00000374383, ENST00000465499, ENST00000602447, ENST00000602978, ENST00000684092, ENST00000855863, ENST00000855864, ENST00000932780, ENST00000932781, ENST00000932782, ENST00000967701, ENST00000967702, ENST00000967703

RefSeq mRNA: 4 — MANE Select: NM_001364929 NM_001363756, NM_001364929, NM_001364930, NM_001364931

CCDS: CCDS87673, CCDS94456

Canonical transcript exons

ENST00000684092 — 50 exons

Exon	Start	End
ENSE00000720073	111363588	111363659
ENSE00000720075	111366239	111366327
ENSE00000720082	111370435	111370627
ENSE00000720085	111370722	111370765
ENSE00000720190	111420017	111420120
ENSE00000720194	111421921	111422043
ENSE00000720197	111422134	111422200
ENSE00000806117	111417883	111418006
ENSE00000806118	111423199	111423248
ENSE00001364494	111442306	111442424
ENSE00001367049	111430547	111430628
ENSE00001368357	111451425	111451555
ENSE00001369993	111444378	111444494
ENSE00001376162	111440372	111440521
ENSE00001383492	111433233	111433372
ENSE00001383777	111436940	111437108
ENSE00001389082	111428042	111428161
ENSE00001419591	111425418	111425496
ENSE00001423748	111425743	111425828
ENSE00001463465	111472897	111473000
ENSE00001630230	111412014	111412148
ENSE00001743907	111413895	111413986
ENSE00001749591	111410041	111410213
ENSE00001750168	111410980	111411142
ENSE00001768316	111414429	111414651
ENSE00001790887	111416272	111416352
ENSE00003469777	111369035	111369173
ENSE00003473072	111389556	111389723
ENSE00003478420	111373170	111373236
ENSE00003500191	111394160	111394305
ENSE00003537610	111373315	111373406
ENSE00003547721	111366522	111366627
ENSE00003554775	111397030	111397153
ENSE00003557551	111392768	111392882
ENSE00003585514	111391756	111391824
ENSE00003609697	111389984	111390101
ENSE00003610260	111385337	111385442
ENSE00003611311	111378580	111378730
ENSE00003618161	111371621	111371829
ENSE00003636511	111384522	111384569
ENSE00003637896	111375113	111375202
ENSE00003640171	111393680	111393734
ENSE00003641180	111386377	111386456
ENSE00003656577	111376476	111376541
ENSE00003664642	111372429	111372620
ENSE00003680110	111373972	111374038
ENSE00003686389	111383211	111383332
ENSE00003785668	111408571	111408672
ENSE00003920599	111484116	111484383
ENSE00003920851	111360685	111362169

Expression profiles

Bgee: expression breadth ubiquitous, 296 present calls, max score 98.54.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 52.0410 / max 307.7590, expressed in 1825 samples.

FANTOM5 promoters (15 alternative TSS)

Promoter ID	TPM avg	Samples expressed
102013	29.0780	1813
101997	8.4150	1711
102014	6.1124	1725
102005	4.3598	1582
102006	0.8713	590
102004	0.7701	396
101999	0.6132	314
102008	0.5733	337
102007	0.3118	118
101998	0.2593	101

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
gastrocnemius	UBERON:0001388	98.54	gold quality
tendon of biceps brachii	UBERON:0008188	98.30	gold quality
buccal mucosa cell	CL:0002336	98.26	gold quality
muscle of leg	UBERON:0001383	98.26	gold quality
hindlimb stylopod muscle	UBERON:0004252	98.24	gold quality
gluteal muscle	UBERON:0002000	98.09	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	97.93	gold quality
skeletal muscle tissue	UBERON:0001134	97.55	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	97.54	gold quality
muscle organ	UBERON:0001630	97.50	gold quality
skeletal muscle organ	UBERON:0014892	97.50	gold quality
deltoid	UBERON:0001476	97.44	gold quality
biceps brachii	UBERON:0001507	97.38	gold quality
medial globus pallidus	UBERON:0002477	97.31	gold quality
endothelial cell	CL:0000115	97.02	gold quality
body of tongue	UBERON:0011876	97.01	gold quality
globus pallidus	UBERON:0001875	96.99	gold quality
substantia nigra pars compacta	UBERON:0001965	96.93	gold quality
substantia nigra pars reticulata	UBERON:0001966	96.93	gold quality
sperm	CL:0000019	96.77	gold quality
tibialis anterior	UBERON:0001385	96.77	gold quality
triceps brachii	UBERON:0001509	96.67	gold quality
lateral globus pallidus	UBERON:0002476	96.61	gold quality
male germ cell	CL:0000015	96.55	gold quality
muscle tissue	UBERON:0002385	96.55	gold quality
epithelium of nasopharynx	UBERON:0001951	96.39	gold quality
tendon	UBERON:0000043	96.33	gold quality
tongue	UBERON:0001723	96.30	gold quality
stromal cell of endometrium	CL:0002255	96.20	gold quality
diaphragm	UBERON:0001103	96.16	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	8.38
E-MTAB-6142	no	132.30

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

75 targeting ECPAS, 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-5692A	100.00	74.40	6850
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502
HSA-MIR-548B-5P	99.94	71.23	3502
HSA-MIR-548BB-5P	99.94	71.27	3509
HSA-MIR-548C-5P	99.94	71.24	3488
HSA-MIR-548D-5P	99.94	71.23	3502
HSA-MIR-548H-5P	99.94	71.24	3488
HSA-MIR-548I	99.94	71.25	3481
HSA-MIR-548J-5P	99.94	71.14	3489
HSA-MIR-548O-5P	99.94	71.24	3488
HSA-MIR-548W	99.94	71.24	3488
HSA-MIR-548Y	99.94	71.28	3514

Literature-anchored findings (GeneRIF, showing 5)

• Ecm29 protein serves to couple the 26 S proteasome to secretory compartments engaged in quality control and to other sites of enhanced proteolysis (PMID:15496406)
• Ecm29 serves as an adaptor for coupling 26 S proteasomes to specific cellular compartments. (PMID:20682791)
• The absence of Ecm29 enhanced TLR3 signaling, which was characterized by the increased abundance of the adaptor protein and E3 ubiquitin ligase tumor necrosis factor receptor-associated factor 3 (PMID:24084648)
• Ecm29 is involved in the dissociation process of 26S proteasome, providing clue to analyse the mechanism of proteasomal degradation under various stress condition. (PMID:26802743)
• Data suggest that the adapter protein ECM29 is the main proteasome-interacting protein responsible for oxidative stress-induced proteasome disassembly/remodeling; ECM29 appears to intrude on interaction between the 20S core particle and 19S regulatory particle in 26S proteasome, disrupting proteasome structure in response to oxidative stress. (PMID:28821611)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	ecpas	ENSDARG00000061952
mus_musculus	Ecpas	ENSMUSG00000050812
rattus_norvegicus	Ecpas	ENSRNOG00000025076
drosophila_melanogaster	CG8858	FBGN0033698
caenorhabditis_elegans		WBGENE00008422

Paralogs (1): GCN1 (ENSG00000089154)

Protein

Protein identifiers

Proteasome adapter and scaffold protein ECM29 — Q5VYK3 (reviewed: Q5VYK3)

Alternative names: Ecm29 proteasome adapter and scaffold, Proteasome-associated protein ECM29 homolog

All UniProt accessions (6): A0AAA9X0G7, F6XAQ5, Q5VYK3, J3KN16, R4GMY1, R4GMY3

UniProt curated annotations — full annotation on UniProt →

Function. Adapter/scaffolding protein that binds to the 26S proteasome, motor proteins and other compartment specific proteins. May couple the proteasome to different compartments including endosome, endoplasmic reticulum and centrosome. May play a role in ERAD and other enhanced proteolysis. Promotes proteasome dissociation under oxidative stress.

Subunit / interactions. Non-stoichiometric component of the proteasome; associates with the 26S proteasome. Interacts (via N-terminus) with VPS11, VPS26A, VPS36, RAB11FIP4 and RABEP1. Interacts (via C-terminus) with DCTN1, DCTN2, KIF5B, MYH7, MYH10, MYO10 and ARF6.

Subcellular location. Endoplasmic reticulum. Endoplasmic reticulum-Golgi intermediate compartment. Endosome. Cytoplasm. Cytoskeleton. Microtubule organizing center. Centrosome. Nucleus. Multivesicular body. Cytoplasmic vesicle.

Similarity. Belongs to the ECM29 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q5VYK3-1	1	yes
Q5VYK3-2	2

RefSeq proteins (4): NP_001350685, NP_001351858, NP_001351859, NP_001351860 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR011989	ARM-like	Homologous_superfamily
IPR016024	ARM-type_fold	Homologous_superfamily
IPR024372	Ecm29_N	Domain
IPR055443	HEAT_ECM29	Domain
IPR055444	ARM_ECM29	Domain

Pfam: PF12755, PF13001, PF23702, PF23731, PF24492

UniProt features (38 total): repeat 27, modified residue 3, initiator methionine 1, chain 1, region of interest 1, compositionally biased region 1, cross-link 1, splice variant 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q5VYK3-F1	84.03	0.40

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 (4): 2, 830, 836, 1039

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 135 (showing top): GOBP_RESPONSE_TO_NITROGEN_COMPOUND, MODULE_151, GOBP_RESPONSE_TO_ENDOPLASMIC_RETICULUM_STRESS, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_PROTEASOME_ASSEMBLY, GOCC_MICROTUBULE_ORGANIZING_CENTER, GOCC_TRANS_GOLGI_NETWORK, GOCC_COATED_VESICLE, GOCC_CENTROSOME, JAATINEN_HEMATOPOIETIC_STEM_CELL_UP, CUI_TCF21_TARGETS_2_DN, GOBP_PROTEASOMAL_PROTEIN_CATABOLIC_PROCESS, HAN_SATB1_TARGETS_DN, GOBP_ERAD_PATHWAY, GOBP_PROTEIN_CATABOLIC_PROCESS

GO Biological Process (2): ERAD pathway (GO:0036503), proteasome assembly (GO:0043248)

GO Molecular Function (3): molecular adaptor activity (GO:0060090), proteasome binding (GO:0070628), protein binding (GO:0005515)

GO Cellular Component (16): proteasome complex (GO:0000502), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), early endosome (GO:0005769), late endosome (GO:0005770), multivesicular body (GO:0005771), endoplasmic reticulum (GO:0005783), endoplasmic reticulum-Golgi intermediate compartment (GO:0005793), centrosome (GO:0005813), membrane (GO:0016020), COPII-coated ER to Golgi transport vesicle (GO:0030134), endocytic vesicle (GO:0030139), cytoplasmic vesicle (GO:0031410), endosome (GO:0005768), cytoskeleton (GO:0005856)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
intracellular membrane-bounded organelle	3
cellular anatomical structure	3
cytoplasm	3
binding	2
endosome	2
endomembrane system	2
cytoplasmic vesicle	2
proteasomal protein catabolic process	1
response to endoplasmic reticulum stress	1
response to chemical	1
protein-containing complex assembly	1
molecular_function	1
protein-containing complex binding	1
intracellular protein-containing complex	1
endopeptidase complex	1
nuclear lumen	1
intracellular anatomical structure	1
late endosome	1
centriole	1
microtubule organizing center	1
coated vesicle	1
intracellular vesicle	1
intracellular membraneless organelle	1

Protein interactions and networks

STRING

1082 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ECPAS	CNOT4	O95628	771
ECPAS	PSME4	Q14997	736
ECPAS	POMP	Q9Y244	726
ECPAS	PSMD4	P55036	718
ECPAS	PSME3	P61289	627
ECPAS	PSMD14	O00487	624
ECPAS	ADRM1	Q16186	611
ECPAS	USP14	P54578	607
ECPAS	PSMD8	P48556	587
ECPAS	PAAF1	Q9BRP4	577
ECPAS	PSMD12	O00232	557
ECPAS	PSMC4	P43686	530
ECPAS	CADPS2	Q86UW7	527
ECPAS	PSMA3	P25788	522
ECPAS	PSMF1	Q92530	506

IntAct

220 interactions, top by confidence:

A	B	Type	Score
HRAS	RAF1	psi-mi:“MI:0914”(association)	0.980
TOLLIP	TOM1	psi-mi:“MI:0914”(association)	0.890
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
VMA12	ATP6AP2	psi-mi:“MI:0914”(association)	0.640
PSMB7	PSMD11	psi-mi:“MI:0914”(association)	0.640
AGTRAP	ECPAS	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	CMTM5	psi-mi:“MI:0915”(physical association)	0.560
CMTM5	ECPAS	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	MAL2	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	AGTRAP	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	DGAT2L6	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	HSD17B13	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	BSND	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	TNFRSF10D	psi-mi:“MI:0915”(physical association)	0.560
ECPAS	CMTM6	psi-mi:“MI:0915”(physical association)	0.560
HTR2C	KLRG2	psi-mi:“MI:0914”(association)	0.530
MAS1	POTEF	psi-mi:“MI:0914”(association)	0.530
SLC2A5	RBFOX3	psi-mi:“MI:0914”(association)	0.530
APLNR	METTL15	psi-mi:“MI:0914”(association)	0.530
IL13RA2	METTL15	psi-mi:“MI:0914”(association)	0.530
NPY2R	RTL8C	psi-mi:“MI:0914”(association)	0.530

BioGRID (420): AGTRAP (Two-hybrid), CMTM5 (Two-hybrid), KIAA0368 (Affinity Capture-MS), KIAA0368 (Affinity Capture-MS), KIAA0368 (Affinity Capture-MS), KIAA0368 (Affinity Capture-MS), KIAA0368 (Affinity Capture-MS), KIAA0368 (Affinity Capture-MS), KIAA0368 (Two-hybrid), KIAA0368 (Two-hybrid), CDKN2AIP (Co-fractionation), DDX1 (Co-fractionation), DNAJB1 (Co-fractionation), DNAJB4 (Co-fractionation), EIF4H (Co-fractionation)

ESM2 similar proteins: A0A0R4ITC5, A1L1F4, A4L9P7, E9Q8I9, F1MKX4, F1QFR9, F1R2X6, F8VPU6, O94915, P21359, P42345, P42346, P51593, P97526, Q04690, Q14997, Q29RF7, Q2HJG5, Q498H0, Q4KLU7, Q4QXM3, Q4VA53, Q5F3U9, Q5F3V3, Q5R6J0, Q5SSW2, Q5TBA9, Q5U241, Q5VYK3, Q6A026, Q6DDM4, Q6GP04, Q6NRP2, Q6P4S8, Q6PDI5, Q6TRW4, Q7PX35, Q7TMY8, Q7Z3U7, Q7Z6Z7

Diamond homologs: Q5R6J0, Q5VYK3, Q6PDI5, Q9V677

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 210 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
Cross-presentation of soluble exogenous antigens (endosomes)	7	12.8×	2e-04
Regulation of RAS by GAPs	9	12.5×	2e-05
AUF1 (hnRNP D0) binds and destabilizes mRNA	7	12.5×	2e-04
Regulation of activated PAK-2p34 by proteasome mediated degradation	6	12.0×	5e-04
Regulation of ornithine decarboxylase (ODC)	6	11.7×	5e-04
SPOP-mediated proteasomal degradation of PD-L1(CD274)	7	11.5×	2e-04
Vpu mediated degradation of CD4	6	11.5×	5e-04
Autodegradation of the E3 ubiquitin ligase COP1	6	11.5×	5e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	300
Likely benign	8
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

7777 predictions. Top by Δscore:

Variant	Effect	Δscore
9:111366235:TCACC:T	donor_loss	1.0000
9:111366236:CA:C	donor_loss	1.0000
9:111366237:A:T	donor_loss	1.0000
9:111366323:TTAAC:T	acceptor_gain	1.0000
9:111366324:TAAC:T	acceptor_gain	1.0000
9:111366326:ACC:A	acceptor_loss	1.0000
9:111366327:CC:C	acceptor_loss	1.0000
9:111366327:CCTA:C	acceptor_gain	1.0000
9:111366328:C:CC	acceptor_gain	1.0000
9:111366328:C:CG	acceptor_loss	1.0000
9:111366329:T:A	acceptor_loss	1.0000
9:111366338:C:CT	acceptor_gain	1.0000
9:111366339:A:T	acceptor_gain	1.0000
9:111366520:ACC:A	donor_gain	1.0000
9:111366521:CCC:C	donor_gain	1.0000
9:111369030:CTTAC:C	donor_loss	1.0000
9:111369031:TTA:T	donor_loss	1.0000
9:111369032:TAC:T	donor_loss	1.0000
9:111369033:A:AC	donor_gain	1.0000
9:111369033:ACG:A	donor_loss	1.0000
9:111369034:C:A	donor_loss	1.0000
9:111369034:C:CC	donor_gain	1.0000
9:111369034:CG:C	donor_gain	1.0000
9:111369034:CGT:C	donor_gain	1.0000
9:111369169:GAGTT:G	acceptor_gain	1.0000
9:111369170:AGTT:A	acceptor_gain	1.0000
9:111369171:GTT:G	acceptor_gain	1.0000
9:111369172:TT:T	acceptor_gain	1.0000
9:111369172:TTC:T	acceptor_loss	1.0000
9:111369174:C:CC	acceptor_gain	1.0000

AlphaMissense

11988 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000001333 (9:111369593 T>C), RS1000028108 (9:111396228 T>C), RS1000036107 (9:111387011 G>C), RS1000065154 (9:111459212 T>C), RS1000091566 (9:111439323 C>T), RS1000131015 (9:111368478 T>C), RS1000136726 (9:111434498 T>C), RS1000158231 (9:111465409 G>A,C), RS1000211076 (9:111451701 A>C), RS1000214991 (9:111462193 T>A), RS1000257774 (9:111419674 G>T), RS1000305956 (9:111451154 A>C,G), RS1000330705 (9:111416679 G>A), RS1000331076 (9:111473601 C>T), RS1000393931 (9:111432352 G>A)

Disease associations

OMIM: gene MIM:616694 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST003994_3	Age at voice drop	1.000000e-07
GCST004750_22	Squamous cell lung carcinoma	5.000000e-06
GCST009391_691	Metabolite levels	8.000000e-06
GCST90002387_342	Immature fraction of reticulocytes	1.000000e-09

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0007888	age at voice drop
EFO:0008529	kynurenine measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4295853 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 4 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.94	Kd	1151	nM	CHEMBL5653589
5.94	ED50	1151	nM	CHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 5 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	2148282: Binding affinity to human ECM29 incubated for 45 mins by Kinobead based pull down assay	kd	1.1505	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression, increases methylation	9
bisphenol A	increases expression, affects expression, decreases expression	3
trichostatin A	decreases expression, increases expression, affects expression	2
entinostat	decreases expression, affects cotreatment	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	2
Panobinostat	affects cotreatment, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
Tretinoin	decreases expression	2
Cyclosporine	increases expression	2
aristolochic acid I	decreases expression	1
FR900359	increases phosphorylation	1
methylmercuric chloride	increases expression, decreases expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, decreases expression, increases abundance	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, affects localization, decreases expression, increases expression	1
arsenite	affects binding, decreases reaction	1
butyraldehyde	decreases expression	1
perfluorooctanoic acid	increases expression	1
methacrylaldehyde	affects cotreatment, decreases expression, increases abundance	1
pentanal	decreases expression	1
di-n-butylphosphoric acid	affects expression	1
2,3,5-(triglutathion-S-yl)hydroquinone	decreases ADP-ribosylation, increases ADP-ribosylation	1
2-palmitoylglycerol	increases expression	1
nutlin 3	affects cotreatment, increases secretion	1
bisphenol B	increases expression	1
dorsomorphin	decreases expression, affects cotreatment	1
hexabrominated diphenyl ether 153	decreases expression	1
bisphenol S	increases expression	1
LDN 193189	affects cotreatment, decreases expression	1

ChEMBL screening assays

2 unique, capped per target: 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4119005	Binding	Binding affinity to KIAA0368 in human NCI-H358 cells at 1 uM by mass spectrometry based pull down assay	Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. — Bioorg Med Chem

Clinical trials (associated diseases)

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