CHERP

Summary

CHERP (calcium homeostasis endoplasmic reticulum protein, HGNC:16930) is a protein-coding gene on chromosome 19p13.11, encoding Calcium homeostasis endoplasmic reticulum protein (Q8IWX8). Involved in calcium homeostasis, growth and proliferation. It is a common-essential gene (DepMap: required in 99.8% of cancer cell lines).

Enables transmembrane transporter binding activity. Involved in positive regulation of calcineurin-NFAT signaling cascade and release of sequestered calcium ion into cytosol. Acts upstream of or within intracellular calcium ion homeostasis and negative regulation of cell population proliferation. Located in perinuclear region of cytoplasm.

Source: NCBI Gene 10523 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 82 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 99.8% of screened cell lines (common-essential)
• MANE Select transcript: NM_006387

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:16930
Approved symbol	CHERP
Name	calcium homeostasis endoplasmic reticulum protein
Location	19p13.11
Locus type	gene with protein product
Status	Approved
Aliases	ERPROT213-21, DAN16
Ensembl gene	ENSG00000085872
Ensembl biotype	protein_coding
OMIM	618539
Entrez	10523

Gene structure

Transcript identifiers

Ensembl transcripts: 20 — 15 protein_coding, 4 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000198939, ENST00000544299, ENST00000546361, ENST00000546538, ENST00000551747, ENST00000597261, ENST00000600432, ENST00000862398, ENST00000862399, ENST00000862400, ENST00000862401, ENST00000862402, ENST00000862403, ENST00000862404, ENST00000862405, ENST00000862406, ENST00000936594, ENST00000936595, ENST00000936596, ENST00000936597

RefSeq mRNA: 1 — MANE Select: NM_006387 NM_006387

CCDS: CCDS42518

Canonical transcript exons

ENST00000546361 — 17 exons

Exon	Start	End
ENSE00000687040	16529648	16529900
ENSE00000687043	16530585	16530674
ENSE00000873470	16528080	16528255
ENSE00000873473	16530769	16530880
ENSE00000873474	16532598	16532749
ENSE00001368832	16541870	16542043
ENSE00002359603	16542354	16542437
ENSE00002395020	16517894	16519352
ENSE00003493310	16535452	16535636
ENSE00003515488	16521521	16521654
ENSE00003518605	16520826	16520912
ENSE00003542976	16525242	16525677
ENSE00003559233	16519621	16519715
ENSE00003570521	16533011	16533148
ENSE00003576469	16520149	16520265
ENSE00003635090	16523052	16523290
ENSE00003666164	16520364	16520507

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 97.95.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 53.4470 / max 327.5984, expressed in 1825 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
179813	52.1536	1824
179814	0.5571	251
179811	0.3778	199
179812	0.3533	192
179809	0.0052	1

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	97.95	gold quality
oocyte	CL:0000023	96.64	gold quality
Brodmann (1909) area 23	UBERON:0013554	94.59	gold quality
right uterine tube	UBERON:0001302	93.88	gold quality
adult organism	UBERON:0007023	93.86	gold quality
epithelium of nasopharynx	UBERON:0001951	93.65	gold quality
right hemisphere of cerebellum	UBERON:0014890	93.39	gold quality
amniotic fluid	UBERON:0000173	93.28	gold quality
tibia	UBERON:0000979	93.11	gold quality
left ovary	UBERON:0002119	92.95	gold quality
cerebellar hemisphere	UBERON:0002245	92.75	gold quality
cerebellar cortex	UBERON:0002129	92.64	gold quality
primary visual cortex	UBERON:0002436	92.62	gold quality
ovary	UBERON:0000992	92.58	gold quality
pituitary gland	UBERON:0000007	92.46	gold quality
endometrium epithelium	UBERON:0004811	92.46	gold quality
right lobe of thyroid gland	UBERON:0001119	92.43	gold quality
adenohypophysis	UBERON:0002196	92.34	gold quality
right testis	UBERON:0004534	92.34	gold quality
left testis	UBERON:0004533	92.31	gold quality
right ovary	UBERON:0002118	92.25	gold quality
cerebellum	UBERON:0002037	92.23	gold quality
right lobe of liver	UBERON:0001114	92.19	gold quality
parietal pleura	UBERON:0002400	92.18	gold quality
lower esophagus mucosa	UBERON:0035834	92.14	gold quality
gingival epithelium	UBERON:0001949	92.08	gold quality
left lobe of thyroid gland	UBERON:0001120	92.04	gold quality
visceral pleura	UBERON:0002401	92.04	gold quality
epithelium of mammary gland	UBERON:0003244	91.76	gold quality
cartilage tissue	UBERON:0002418	91.75	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.87

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

46 targeting CHERP, 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-4455	100.00	65.48	1587
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-539-3P	99.98	70.74	1616
HSA-MIR-485-3P	99.98	70.68	1585
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-551B-5P	99.96	71.28	3493
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-6508-5P	99.92	70.67	2465
HSA-MIR-8063	99.91	69.76	3146
HSA-MIR-9902	99.89	69.15	2250
HSA-MIR-605-3P	99.88	69.22	1833
HSA-MIR-8067	99.86	69.59	2260
HSA-MIR-5010-3P	99.83	70.60	2357
HSA-MIR-3180-5P	99.82	69.12	2422
HSA-MIR-3680-3P	99.75	72.51	3095
HSA-MIR-12130	99.75	65.47	452
HSA-MIR-33A-3P	99.70	70.27	3362
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-6126	99.62	68.09	996
HSA-MIR-7152-5P	99.60	69.33	2094
HSA-MIR-154-3P	99.50	70.05	831
HSA-MIR-487A-3P	99.50	69.95	840
HSA-MIR-203A-3P	99.49	70.56	2806

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.8% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 4)

• CHERP is an RyR1 interacting protein that may be involved in the regulation of excitation-contraction coupling (PMID:21454501)
• analysis of the role of calcium homeostasis endoplasmic reticulum protein (CHERP) in cellular calcium signaling (PMID:23148228)
• CHERP and ALG-2 participate in regulation of alternative splicing of IP3R1 pre-mRNA and provide new insights into post-transcriptional regulation of splicing variants in Ca(2+) signaling pathways. (PMID:24078636)
• Study observed that CHERP and its binding partner SR140 are significantly upregulated in human clinical colorectal cancer tissues (CRC) and clarified how CHERP/SR140 exert an oncogenic role in CRC development partially through regulating expression of UPF3A variants. (PMID:30977118)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	cherp	ENSDARG00000021812
mus_musculus	Cherp	ENSMUSG00000052488
rattus_norvegicus	Cherp	ENSRNOG00000012323
drosophila_melanogaster	scaf6	FBGN0261872
caenorhabditis_elegans		WBGENE00006442

Protein

Protein identifiers

Calcium homeostasis endoplasmic reticulum protein — Q8IWX8 (reviewed: Q8IWX8)

Alternative names: ERPROT 213-21, SR-related CTD-associated factor 6

All UniProt accessions (2): Q8IWX8, J3QK89

UniProt curated annotations — full annotation on UniProt →

Function. Involved in calcium homeostasis, growth and proliferation.

Subcellular location. Cytoplasm. Perinuclear region. Endoplasmic reticulum.

Tissue specificity. Expressed in brain, placenta, lung, liver, kidney, pancreas, cardiac and skeletal muscle, and in cultured HEL and Dami cells.

RefSeq proteins (1): NP_006378* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000061	Surp	Domain
IPR000467	G_patch_dom	Domain
IPR006569	CID_dom	Domain
IPR008942	ENTH_VHS	Homologous_superfamily
IPR035967	SWAP/Surp_sf	Homologous_superfamily
IPR056721	DUF7819	Domain

Pfam: PF01585, PF01805, PF04818, PF25127

UniProt features (37 total): modified residue 12, sequence conflict 9, compositionally biased region 6, region of interest 3, domain 2, cross-link 2, chain 1, repeat 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8IWX8-F1	63.55	0.24

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 (14): 1, 18, 714, 813, 815, 817, 819, 828, 855, 857, 879, 904, 844, 872

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-72163	mRNA Splicing - Major Pathway
R-HSA-9770562	mRNA Polyadenylation
R-HSA-9918481	Dengue Virus-Host Interactions
R-HSA-9943411	CHD1 and CHD2 subfamily

MSigDB gene sets: 152 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_UP, MORF_ESPL1, GOBP_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING, MORF_SMC1L1, YAO_HOXA10_TARGETS_VIA_PROGESTERONE_UP, MORF_RRM1, MORF_HDAC1, MORF_UBE2N, MORF_HDAC2, SHEPARD_BMYB_MORPHOLINO_DN, GOBP_MONOATOMIC_CATION_TRANSPORT, PUJANA_CHEK2_PCC_NETWORK, SHEDDEN_LUNG_CANCER_GOOD_SURVIVAL_A5, GCM_PRKCG, GOBP_POSITIVE_REGULATION_OF_CALCIUM_MEDIATED_SIGNALING

GO Biological Process (6): RNA processing (GO:0006396), intracellular calcium ion homeostasis (GO:0006874), nervous system development (GO:0007399), negative regulation of cell population proliferation (GO:0008285), release of sequestered calcium ion into cytosol (GO:0051209), positive regulation of calcineurin-NFAT signaling cascade (GO:0070886)

GO Molecular Function (4): RNA binding (GO:0003723), transmembrane transporter binding (GO:0044325), nucleic acid binding (GO:0003676), protein binding (GO:0005515)

GO Cellular Component (6): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), membrane (GO:0016020), sarcoplasmic reticulum membrane (GO:0033017), perinuclear region of cytoplasm (GO:0048471), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
mRNA Splicing	1
mRNA 3’-end processing	1
Dengue Virus Infection	1
CHD chromatin remodelers	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
binding	2
cytoplasm	2
gene expression	1
RNA biosynthetic process	1
primary metabolic process	1
intracellular monoatomic cation homeostasis	1
calcium ion homeostasis	1
system development	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
intercellular transport	1
calcium ion transmembrane import into cytosol	1
calcineurin-NFAT signaling cascade	1
regulation of calcineurin-NFAT signaling cascade	1
positive regulation of calcineurin-mediated signaling	1
nucleic acid binding	1
protein binding	1
nuclear lumen	1
intracellular anatomical structure	1
endoplasmic reticulum membrane	1
sarcoplasmic reticulum	1
bounding membrane of organelle	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1428 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CHERP	U2SURP	O15042	853
CHERP	RBM17	Q96I25	785
CHERP	SF1	Q15637	618
CHERP	PLSCR3	Q9NRY6	607
CHERP	SF3A2	Q15428	519
CHERP	CCDC97	Q96F63	505
CHERP	NR2C2AP	Q86WQ0	491
CHERP	SLC35E1	Q96K37	472
CHERP	CIB3	Q96Q77	453
CHERP	SHISA4	Q96DD7	433
CHERP	EFCC1	Q9HA90	429
CHERP	DHX8	Q14562	422
CHERP	GPATCH11	Q8N954	422
CHERP	PATL1	Q86TB9	420
CHERP	NCLN	Q969V3	415

IntAct

270 interactions, top by confidence:

A	B	Type	Score
SF1	U2AF2	psi-mi:“MI:0914”(association)	0.950
SNRPF	GEMIN2	psi-mi:“MI:0914”(association)	0.910
LARP7	CCNT1	psi-mi:“MI:0914”(association)	0.850
RBM17	U2SURP	psi-mi:“MI:0914”(association)	0.740
COMMD4	VPS26C	psi-mi:“MI:0914”(association)	0.730
PPP1CA	CCDC85C	psi-mi:“MI:0914”(association)	0.670
PPP1CA	CCDC85C	psi-mi:“MI:2364”(proximity)	0.670
SNRPB	PRMT5	psi-mi:“MI:0914”(association)	0.670
NCBP2	KPNA3	psi-mi:“MI:0914”(association)	0.640
COMMD6	VPS26C	psi-mi:“MI:0914”(association)	0.640
LIN28A	IGF2BP3	psi-mi:“MI:0914”(association)	0.640
SNRPA1	U2SURP	psi-mi:“MI:0914”(association)	0.640
CHERP	SF1	psi-mi:“MI:0407”(direct interaction)	0.580
U2SURP	CHERP	psi-mi:“MI:0915”(physical association)	0.560
CHERP	CLK3	psi-mi:“MI:0915”(physical association)	0.560
FIGN	CHERP	psi-mi:“MI:0915”(physical association)	0.560
LASP1	CHERP	psi-mi:“MI:0915”(physical association)	0.560
TLE3	CHERP	psi-mi:“MI:0915”(physical association)	0.560
CHERP	SAXO1	psi-mi:“MI:0915”(physical association)	0.560
C1orf94	CHERP	psi-mi:“MI:0915”(physical association)	0.560
ADAMTSL4	CHERP	psi-mi:“MI:0915”(physical association)	0.560
RBFOX2	CHERP	psi-mi:“MI:0915”(physical association)	0.560
CHERP	MAGED1	psi-mi:“MI:0915”(physical association)	0.560
SORBS3	CHERP	psi-mi:“MI:0915”(physical association)	0.560
FASTK	CHERP	psi-mi:“MI:0915”(physical association)	0.560
KRTAP11-1	CHERP	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (373): CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), U2SURP (Co-fractionation), CHERP (Affinity Capture-RNA), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS), CHERP (Affinity Capture-MS)

ESM2 similar proteins: A0A3B3IU46, A0JMU8, A1L1K8, A2RV70, O94432, P07733, P45978, P46553, P90897, Q09801, Q09911, Q14444, Q1LZB6, Q24669, Q28F29, Q28HC9, Q2HJG4, Q5CZI8, Q5JVS0, Q5M9G3, Q5R9Q6, Q5UR41, Q5ZMS6, Q60865, Q66HC1, Q6CVS3, Q6FJC7, Q6NRP6, Q6NRY1, Q6NYG6, Q6P0F4, Q6P1U3, Q75A59, Q8CGZ0, Q8IWX8, Q8TAP9, Q8VDM6, Q91W18, Q9BTL3, Q9BUJ2

Diamond homologs: A2VDN6, B9DHA6, G1SK22, O13900, O14399, O15042, P05759, P0C016, P0C030, P0C031, P0C032, P0C073, P0C8R3, P0CG71, P0CG73, P0CG81, P0CG82, P0CG83, P0CG84, P0CG85, P0CG86, P0CG87, P0CH04, P0CH05, P0CH10, P0CH11, P0CH27, P0CH32, P0CH33, P0CH34, P0CH35, P0DJ25, P12297, P14795, P14799, P15357, P19848, P23324, P23398, P27923

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 192 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
Metabolism of non-coding RNA	7	33.6×	2e-08
SARS-CoV-2 modulates host translation machinery	13	22.1×	1e-12
mRNA Splicing - Minor Pathway	12	20.4×	3e-11
Transport of Mature Transcript to Cytoplasm	7	20.2×	6e-07
RNA Polymerase II Transcription Termination	12	20.0×	3e-11
Eukaryotic Translation Initiation	8	18.7×	1e-07
Cap-dependent Translation Initiation	8	18.7×	1e-07
SARS-CoV-1 modulates host translation machinery	8	18.7×	1e-07

GO biological processes:

GO term	Partners	Fold	FDR
U2-type prespliceosome assembly	9	32.9×	1e-09
negative regulation of DNA recombination	5	32.9×	3e-05
chromosome condensation	6	29.6×	4e-06
alternative mRNA splicing, via spliceosome	7	27.6×	6e-07
spliceosomal complex assembly	7	24.6×	1e-06
negative regulation of mRNA splicing, via spliceosome	5	22.4×	2e-04
spliceosomal snRNP assembly	6	20.4×	4e-05
RNA splicing, via transesterification reactions	5	18.2×	4e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	65
Likely benign	5
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

3299 predictions. Top by Δscore:

Variant	Effect	Δscore
19:16519348:CCAGC:C	acceptor_gain	1.0000
19:16519349:CAGC:C	acceptor_gain	1.0000
19:16519349:CAGCC:C	acceptor_gain	1.0000
19:16519351:GCCTG:G	acceptor_loss	1.0000
19:16519352:CCTGG:C	acceptor_loss	1.0000
19:16519353:C:CA	acceptor_loss	1.0000
19:16519353:C:CC	acceptor_gain	1.0000
19:16519619:AC:A	donor_gain	1.0000
19:16519620:CC:C	donor_gain	1.0000
19:16519620:CCCAT:C	donor_gain	1.0000
19:16519624:T:C	donor_gain	1.0000
19:16519715:AC:A	acceptor_loss	1.0000
19:16519716:C:CC	acceptor_gain	1.0000
19:16520110:C:A	donor_gain	1.0000
19:16520133:TAAG:T	donor_gain	1.0000
19:16520134:AAGA:A	donor_gain	1.0000
19:16520147:A:AC	donor_gain	1.0000
19:16520148:C:CC	donor_gain	1.0000
19:16520148:CGG:C	donor_gain	1.0000
19:16520187:T:TA	donor_gain	1.0000
19:16520263:CTT:C	acceptor_gain	1.0000
19:16520273:G:T	donor_gain	1.0000
19:16520503:GTCCG:G	acceptor_gain	1.0000
19:16520504:TCCG:T	acceptor_gain	1.0000
19:16520505:CCG:C	acceptor_gain	1.0000
19:16520505:CCGC:C	acceptor_gain	1.0000
19:16520506:CG:C	acceptor_gain	1.0000
19:16520506:CGC:C	acceptor_gain	1.0000
19:16520506:CGCTG:C	acceptor_gain	1.0000
19:16520507:GC:G	acceptor_loss	1.0000

AlphaMissense

6053 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:16519195:G:C	F905L	1.000
19:16519195:G:T	F905L	1.000
19:16519196:A:C	F905C	1.000
19:16519196:A:G	F905S	1.000
19:16519197:A:G	F905L	1.000
19:16519207:C:A	K901N	1.000
19:16519207:C:G	K901N	1.000
19:16519209:T:C	K901E	1.000
19:16519217:C:G	R898P	1.000
19:16519218:G:T	R898S	1.000
19:16519221:A:C	Y897D	1.000
19:16519257:C:G	G885R	1.000
19:16519314:C:G	G866R	1.000
19:16519314:C:T	G866R	1.000
19:16519348:C:A	W854C	1.000
19:16519348:C:G	W854C	1.000
19:16519349:C:G	W854S	1.000
19:16519350:A:G	W854R	1.000
19:16519350:A:T	W854R	1.000
19:16519621:C:G	G853R	1.000
19:16519632:A:G	L849P	1.000
19:16519632:A:T	L849Q	1.000
19:16519644:C:T	G845D	1.000
19:16519645:C:G	G845R	1.000
19:16520867:T:A	K720N	1.000
19:16520867:T:G	K720N	1.000
19:16520868:T:A	K720I	1.000
19:16520869:T:C	K720E	1.000
19:16520872:C:G	A719P	1.000
19:16520874:C:G	R718P	1.000

dbSNP variants (sampled 300 via entrez): RS1000003678 (19:16543754 G>C), RS1000046955 (19:16530095 G>C), RS1000175285 (19:16533501 T>C), RS1000190575 (19:16534062 T>C), RS1000211722 (19:16539324 T>A,C,G), RS1000242684 (19:16539153 T>A,G), RS1000336264 (19:16529316 C>G), RS1000515340 (19:16534950 C>G), RS1000578314 (19:16538056 C>T), RS1000732572 (19:16543204 T>C), RS1000806460 (19:16530485 C>T), RS1000872294 (19:16529502 G>A,T), RS1001037008 (19:16520681 G>A,C), RS1001073342 (19:16530175 G>A), RS1001177521 (19:16520848 T>G)

Disease associations

OMIM: gene MIM:618539 | 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): CHEMBL5724788 (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)

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
7.16	Kd	70	nM	MOLIBRESIB
6.92	IC50	120	nM	MOLIBRESIB

PubChem BioAssay actives

2 with measured affinity, of 7 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	2179116: Binding affinity against CHERP (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.0700	uM

CTD chemical–gene interactions

26 total (human), top 26 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, increases methylation	2
aristolochic acid I	increases expression	1
FR900359	increases phosphorylation	1
dicrotophos	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases methylation	1
deoxynivalenol	increases expression	1
O,O-diethyl O-3,5,6-trichloro-2-pyridyl phosphate	affects expression, affects response to substance	1
cobaltous chloride	increases expression	1
nivalenol	increases expression	1
2,3,5-(triglutathion-S-yl)hydroquinone	increases ADP-ribosylation	1
Temozolomide	increases expression	1
Vehicle Emissions	increases abundance, increases expression	1
Caffeine	affects phosphorylation	1
Cisplatin	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Estradiol	increases expression	1
Ivermectin	decreases expression	1
Methotrexate	decreases expression	1
Ribonucleotides	affects binding	1
Rotenone	decreases expression	1
Smoke	decreases expression	1
Tetrachlorodibenzodioxin	affects expression	1
Thiram	increases expression	1
Cadmium Chloride	increases expression	1
Particulate Matter	increases abundance, increases expression	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
CHEMBL5697162	Binding	Inhibition of CHERP (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.