COIL

Summary

COIL (coilin, HGNC:2184) is a protein-coding gene on chromosome 17q22, encoding Coilin (P38432). Component of nuclear coiled bodies, also known as Cajal bodies or CBs, which are involved in the modification and assembly of nucleoplasmic snRNPs. It is a selective cancer dependency (DepMap: 17.9% of cell lines).

The protein encoded by this gene is an integral component of Cajal bodies (also called coiled bodies). Cajal bodies are nuclear suborganelles of varying number and composition that are involved in the post-transcriptional modification of small nuclear and small nucleolar RNAs. The N-terminus of the coilin protein directs its self-oligomerization while the C-terminus influences the number of nuclear bodies assembled per cell. Differential methylation and phosphorylation of coilin likely influences its localization among nuclear bodies and the composition and assembly of Cajal bodies. This gene has pseudogenes on chromosome 4 and chromosome 14.

Source: NCBI Gene 8161 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 103 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 17.9% of screened cell lines
• MANE Select transcript: NM_004645

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2184
Approved symbol	COIL
Name	coilin
Location	17q22
Locus type	gene with protein product
Status	Approved
Aliases	CLN80, p80-coilin
Ensembl gene	ENSG00000121058
Ensembl biotype	protein_coding
OMIM	600272
Entrez	8161

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000240316, ENST00000573008, ENST00000873430

RefSeq mRNA: 1 — MANE Select: NM_004645 NM_004645

CCDS: CCDS11592

Canonical transcript exons

ENST00000240316 — 7 exons

Exon	Start	End
ENSE00000820208	56960775	56961050
ENSE00000820211	56949889	56950996
ENSE00000820212	56949681	56949767
ENSE00000820213	56949387	56949434
ENSE00000820214	56946442	56946511
ENSE00000820215	56942035	56942123
ENSE00000820216	56938199	56939154

Expression profiles

Bgee: expression breadth ubiquitous, 287 present calls, max score 99.64.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.6571 / max 203.4393, expressed in 1785 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
167129	16.6571	1785

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sperm	CL:0000019	99.64	gold quality
male germ cell	CL:0000015	98.42	gold quality
buccal mucosa cell	CL:0002336	96.32	gold quality
adult organism	UBERON:0007023	95.11	gold quality
left testis	UBERON:0004533	93.93	gold quality
right testis	UBERON:0004534	93.75	gold quality
testis	UBERON:0000473	93.36	gold quality
hair follicle	UBERON:0002073	92.28	gold quality
esophagus squamous epithelium	UBERON:0006920	92.17	gold quality
epithelium of esophagus	UBERON:0001976	91.47	gold quality
tongue squamous epithelium	UBERON:0006919	90.57	gold quality
tibia	UBERON:0000979	89.69	gold quality
germinal epithelium of ovary	UBERON:0001304	89.40	gold quality
parietal pleura	UBERON:0002400	89.20	gold quality
gingival epithelium	UBERON:0001949	89.08	gold quality
squamous epithelium	UBERON:0006914	89.01	gold quality
urethra	UBERON:0000057	88.69	gold quality
oviduct epithelium	UBERON:0004804	88.66	gold quality
penis	UBERON:0000989	88.39	gold quality
gingiva	UBERON:0001828	88.30	gold quality
palpebral conjunctiva	UBERON:0001812	88.20	gold quality
visceral pleura	UBERON:0002401	87.73	gold quality
pleura	UBERON:0000977	87.61	gold quality
epithelium of mammary gland	UBERON:0003244	87.60	gold quality
secondary oocyte	CL:0000655	87.47	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	87.45	gold quality
mucosa of urinary bladder	UBERON:0001259	87.29	silver quality
eye	UBERON:0000970	87.27	gold quality
amniotic fluid	UBERON:0000173	87.17	gold quality
cartilage tissue	UBERON:0002418	87.15	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.41

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

81 targeting COIL, 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-3163	100.00	77.23	8605
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4425	100.00	67.59	1049
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-4500	99.99	72.72	2367
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-MIR-12136	99.98	72.81	5713
HSA-LET-7D-5P	99.96	71.76	1632
HSA-MIR-4458	99.96	71.64	1650
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-613	99.91	71.50	1710

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 17.9% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 32)

• The level of snRNP protein expression and snRNP assembly, rather than the expression levels of p80-coilin, may be a key trigger for Cajal body formation in stable HeLa cell lines. (PMID:11792806)
• Coilin is a Cajal body marker; its methylation regulates nuclear body formation. (PMID:12361597)
• Specific regions within the C-terminus of coilin, the Cajal Body marker protein, are responsible for regulating the number of nuclear foci. Coilin from various species shows different tendencies to form nuclear foci. (PMID:12482916)
• SMN and coilin interact differentially with Cajal bodies and have roles in the pathway for reassembly of nucleoli and Cajal bodies following mitosis (PMID:12679382)
• p80 coilin protein co-localizes with ataxin-1 aggregates in the nucleoplasm (PMID:12757932)
• specific EB-1/AIDA-1 isoforms, such as AIDA-1c, may participate in the regulation of nucleoplasmic coilin protein interactions in neuronal and transformed cells (PMID:15862129)
• Direct interactions between the Cajal body (CB) protein coilin and the promyelocytic leukemia (PML) body protein PIASy have a role in mediating association of CBs to PML bodies. (PMID:16219678)
• Complexes of proteasome activator subunit gamma/coilin found in Cajal body - levels of complex increased by UV rays. (PMID:17088425)
• Ectopic expression of AGAP2 causes both BRAG2 and the coiled bodies’ marker coilin to accumulate in nucleoli. (PMID:17461797)
• These findings demonstrate that coilin modifications or levels impact artificial reporter splicing, possibly by influencing small nuclear ribonucleoprotein biogenesis. (PMID:18322647)
• FLASH and NPAT positive but not Coilin positive Cajal Bodies correlate with cell ploidy. (PMID:18677100)
• Data support a model whereby coilin is the target of an uncharacterized signal transduction cascade that responds to the increased transcription and snRNP demands found in transformed cells. (PMID:19435804)
• in addition to affecting coilin-coilin interaction and localization in the nucleus, the phosphorylation state of coilin also impacts its interaction with SMN and SmB’ and may play a role in controlling U snRNP cycling through the Cajal bodies. (PMID:19997741)
• results suggest the existence of a dynamic flux of coilin between Cajal bodies, nucleoplasm and nucleolus, and indicate that coilin methylation plays a key role in this process (PMID:20449600)
• Data demonstrate by NMR methods that the carboxy-terminal region contains a Tudor domain. (PMID:20875822)
• Results identify a novel and unexpected function for coilin, independent of its role in snRNP biogenesis, establishing a new link between the DNA damage response and the inhibition of rRNA synthesis. (PMID:21289084)
• These results emphasize the role of coilin phosphorylation in the formation and activity of Cajal bodies. (PMID:21991343)
• The existence of chromatolysis and eccentric nuclei in SMA motor neurons correlates with Cajal body disruption and nucleolar relocalization of coil in, a Cajal body marker. (PMID:22302308)
• new characteristics of coilin in vitro (PMID:22558428)
• investigated the role of coilin in the DNA damage response and found that coilin reduction correlated with significantly increased levels of soluble gammaH2AX in etoposide treated U2OS cells (PMID:22986342)
• coilin is subjected to regulated specific proteolysis by calpain, and this processing may play a role in the regulation of coilin activity and Cajal body formation (PMID:23064547)
• Data indicate coilin involvement in the processing of telomerase RNA both in vitro and in vivo. (PMID:23274112)
• Results suggest that UBL5 could be targeted to Cajal bodies (CBs) via its interaction with coilin. (PMID:23726919)
• The interaction of SMN with the spliceosomal SmD1 (also known as SNRPD1), severely decreases SMN-coilin interaction and prevents Cajal body assembly. (PMID:24413165)
• Data indicate that annexin A2 overexpression in microsatellite instability (MIN) cells induces disassembly and colocalization of coilin with centromeres. (PMID:25347736)
• The study shows that coilin-KO human cells that lack Cajal bodies are phenotypically normal with respect to telomere homeostasis. (PMID:25477378)
• Coilin couples snRNA and snoRNA biogenesis, making cajal bodies the cellular hub of small ncRNA metabolism. (PMID:25514182)
• Authors summarize what has been learned in the past 25 years about coilin’s structure, post-transcriptional modifications, and interactions with RNA and proteins. [Review] (PMID:25970135)
• VRK1 is a novel regulator of CBs dynamics and stability in cell cycle by protecting coilin from ubiquitination and degradation in the proteasome, and propose a model of CB dynamics. (PMID:26068304)
• The Impact of Coilin Nonsynonymous SNP Variants E121K and V145I on Cell Growth and Cajal Body Formation: The First Characterization. (PMID:32764415)
• Coilin enhances phosphorylation and stability of DGCR8 and promotes miRNA biogenesis. (PMID:34319763)
• The Cajal body protein p80-coilin forms a complex with the adenovirus L4-22K protein and facilitates the nuclear export of adenovirus mRNA. (PMID:37795984)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	coil	ENSDARG00000040070
mus_musculus	Coil	ENSMUSG00000033983
rattus_norvegicus	Coil	ENSRNOG00000000244

Protein

Protein identifiers

Coilin — P38432 (reviewed: P38432)

Alternative names: p80-coilin

All UniProt accessions (2): P38432, I3L369

UniProt curated annotations — full annotation on UniProt →

Function. Component of nuclear coiled bodies, also known as Cajal bodies or CBs, which are involved in the modification and assembly of nucleoplasmic snRNPs.

Subunit / interactions. Interacts with ANKS1B. Interacts with SMN1 (via Tudor domain). Interacts (via C-terminus) with AK6. Interacts with WRAP53/TCAB1. Interacts with HMBOX1. Interacts with PSME3; the interaction is inhibited by PSME3IP1. Interacts wit UBL5.

Subcellular location. Nucleus. Cajal body.

Tissue specificity. Found in all the cell types examined.

Post-translational modifications. Symmetrical dimethylation of arginine residues within the RG repeat region enhances affinity for SMN, and thus localization of SMN complexes to CBs. Phosphorylated by VRK1. Phosphorylation during mitosis is associated with disassembly of CBs.

Domain organisation. The atypical Tudor domain at the C-terminus contains two large unstructured loops, and does not bind methylated residues.

Similarity. Belongs to the coilin family.

RefSeq proteins (1): NP_004636* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR024822	Coilin	Family
IPR031722	Coilin_N	Domain
IPR056398	Tudor_Coilin	Domain

Pfam: PF15862, PF23086

UniProt features (48 total): modified residue 16, cross-link 11, repeat 8, region of interest 6, compositionally biased region 4, chain 1, mutagenesis site 1, domain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P38432-F1	59.46	0.22

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 (27): 105, 122, 184, 248, 250, 256, 271, 272, 290, 301, 303, 403, 456, 487, 489, 566, 127, 151, 160, 204 …

Mutagenesis-validated functional residues (1):

Position	Phenotype
413–419	impaired interaction with smn.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 168 (showing top): MORF_MTA1, BROWNE_HCMV_INFECTION_6HR_DN, MORF_RAB5A, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, MORF_RAD21, GENTILE_RESPONSE_CLUSTER_D3, MORF_PSMC2, BROWNE_HCMV_INFECTION_24HR_UP, MORF_SKP1A, MUELLER_PLURINET, GOBP_PROTEIN_RNA_COMPLEX_ORGANIZATION, GOBP_RNA_SPLICING, MORF_PPP6C, GENTILE_UV_HIGH_DOSE_DN

GO Biological Process (1): spliceosomal snRNP assembly (GO:0000387)

GO Molecular Function (4): U1 snRNA binding (GO:0030619), U2 snRNA binding (GO:0030620), identical protein binding (GO:0042802), protein binding (GO:0005515)

GO Cellular Component (7): fibrillar center (GO:0001650), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), Cajal body (GO:0015030), membrane (GO:0016020), nuclear body (GO:0016604)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
snRNA binding	2
nuclear lumen	2
intracellular membraneless organelle	2
mRNA splicing, via spliceosome	1
protein-RNA complex assembly	1
protein binding	1
binding	1
nucleolus	1
intracellular membrane-bounded organelle	1
nuclear ribonucleoprotein granule	1
nucleoplasm	1

Protein interactions and networks

STRING

3236 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
COIL	NOLC1	Q14978	962
COIL	FBL	P22087	935
COIL	SMN1	Q16637	836
COIL	ATXN1	P54253	796
COIL	GEMIN2	O14893	779
COIL	SNRPB	P14678	774
COIL	WRAP53	Q9BUR4	768
COIL	SART3	Q15020	761
COIL	MPHOSPH10	O00566	734
COIL	DKC1	O60832	727
COIL	NPAT	Q14207	722
COIL	LSM11	P83369	721
COIL	PHAX	Q9H814	703
COIL	XRCC6	P12956	682
COIL	SRSF2	Q01130	678

IntAct

355 interactions, top by confidence:

A	B	Type	Score
PIK3CA	PIK3R2	psi-mi:“MI:0914”(association)	0.900
SMN1	SNRPB	psi-mi:“MI:0914”(association)	0.850
BYSL	COIL	psi-mi:“MI:0915”(physical association)	0.840
COIL	BYSL	psi-mi:“MI:0915”(physical association)	0.840
SNRPF	COIL	psi-mi:“MI:0915”(physical association)	0.830
COIL	SNRPF	psi-mi:“MI:0915”(physical association)	0.830
COIL	PSME3	psi-mi:“MI:0915”(physical association)	0.820
VRK1	COIL	psi-mi:“MI:0217”(phosphorylation reaction)	0.680
VRK1	COIL	psi-mi:“MI:0915”(physical association)	0.680
COIL	PDLIM5	psi-mi:“MI:0915”(physical association)	0.670
PDLIM5	COIL	psi-mi:“MI:0915”(physical association)	0.670
COIL	ATXN1	psi-mi:“MI:0915”(physical association)	0.670
ATXN1	COIL	psi-mi:“MI:0915”(physical association)	0.640

BioGRID (654): COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), COIL (Two-hybrid), CDC23 (Two-hybrid), PDLIM5 (Two-hybrid), ZNF277 (Two-hybrid), ARMCX1 (Two-hybrid), ZCCHC10 (Two-hybrid), WDR34 (Two-hybrid), COIL (Co-fractionation)

ESM2 similar proteins: A4FV97, D4ACP5, O09130, O35144, O76021, P38432, P51612, Q01831, Q05CL8, Q08288, Q14684, Q15554, Q28G87, Q32LC1, Q58CQ0, Q58CQ5, Q5I0E6, Q5NC05, Q5NVA9, Q5R8S0, Q5RCE6, Q5RDL2, Q5SU73, Q5SXM2, Q5XI01, Q5ZJJ1, Q66H19, Q66H85, Q6AYK5, Q6IRU7, Q7TSG2, Q80UU1, Q8BJW7, Q8BVY0, Q8N163, Q8VDP4, Q8VID5, Q91VE6, Q91YK2, Q96AY2

Diamond homologs: P38432, Q09003, Q5SU73, Q8RWK8

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
CyclinE/CDK2	up-regulates	COIL	phosphorylation
VRK1	“up-regulates quantity by stabilization”	COIL	phosphorylation
CDK2	up-regulates	COIL	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 87 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
snRNP Assembly	5	19.6×	7e-04
Metabolism of RNA	9	7.0×	7e-04

GO biological processes:

GO term	Partners	Fold	FDR
spliceosomal snRNP assembly	5	42.7×	6e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	87
Likely benign	5
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

932 predictions. Top by Δscore:

Variant	Effect	Δscore
17:56942033:A:AC	donor_gain	1.0000
17:56942033:AC:A	donor_gain	1.0000
17:56942033:ACC:A	donor_loss	1.0000
17:56942034:C:A	donor_loss	1.0000
17:56942034:C:CC	donor_gain	1.0000
17:56942034:CC:C	donor_gain	1.0000
17:56942034:CCTTG:C	donor_gain	1.0000
17:56942119:CAAGG:C	acceptor_gain	1.0000
17:56942120:AAGG:A	acceptor_gain	1.0000
17:56942121:AGG:A	acceptor_gain	1.0000
17:56942121:AGGC:A	acceptor_loss	1.0000
17:56942122:GG:G	acceptor_gain	1.0000
17:56942123:GCTGA:G	acceptor_loss	1.0000
17:56942124:C:CC	acceptor_gain	1.0000
17:56942130:C:CT	acceptor_gain	1.0000
17:56942131:A:T	acceptor_gain	1.0000
17:56942137:A:AC	acceptor_gain	1.0000
17:56942137:A:C	acceptor_gain	1.0000
17:56949382:CTTA:C	donor_loss	1.0000
17:56949384:TA:T	donor_loss	1.0000
17:56949435:C:CC	acceptor_gain	1.0000
17:56960770:CGCAC:C	donor_loss	1.0000
17:56960771:GCACC:G	donor_loss	1.0000
17:56960773:A:AG	donor_loss	1.0000
17:56939151:TGAT:T	acceptor_gain	0.9900
17:56939151:TGATC:T	acceptor_loss	0.9900
17:56939153:ATCTG:A	acceptor_loss	0.9900
17:56939154:TC:T	acceptor_loss	0.9900
17:56939155:C:CC	acceptor_gain	0.9900
17:56939155:CT:C	acceptor_loss	0.9900

AlphaMissense

3734 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:56939142:A:G	W554R	0.999
17:56939142:A:T	W554R	0.999
17:56942101:A:C	F527L	0.999
17:56942101:A:T	F527L	0.999
17:56942103:A:G	F527L	0.999
17:56949685:A:G	F479S	0.999
17:56939132:A:G	L557S	0.998
17:56949387:C:A	K496N	0.998
17:56949387:C:G	K496N	0.998
17:56949684:A:C	F479L	0.998
17:56949684:A:T	F479L	0.998
17:56949686:A:G	F479L	0.998
17:56949688:G:T	A478E	0.998
17:56960823:A:G	L66S	0.998
17:56939119:T:A	R561S	0.997
17:56939119:T:G	R561S	0.997
17:56939140:C:A	W554C	0.997
17:56939140:C:G	W554C	0.997
17:56960981:A:C	F13L	0.997
17:56960981:A:T	F13L	0.997
17:56960983:A:G	F13L	0.997
17:56942096:A:G	L529S	0.996
17:56946501:A:T	I500K	0.996
17:56946507:C:T	G498E	0.996
17:56949681:C:A	K480N	0.996
17:56949681:C:G	K480N	0.996
17:56949721:A:G	L467S	0.996
17:56950994:A:T	V83D	0.996
17:56960898:A:G	L41P	0.996
17:56960941:A:G	W27R	0.996

dbSNP variants (sampled 300 via entrez): RS1000062245 (17:56941919 C>T), RS1000085362 (17:56957299 TA>T,TAA), RS1000137109 (17:56962586 C>G), RS1000290689 (17:56951932 C>T), RS1000431693 (17:56942231 T>C), RS1000580439 (17:56952137 G>A,T), RS1001019814 (17:56956323 C>A), RS1001060913 (17:56939995 T>C,G), RS1001150810 (17:56942554 C>A,T), RS1001233457 (17:56957767 T>C), RS1001411716 (17:56958193 T>C), RS1001461256 (17:56946225 T>C), RS1001577142 (17:56945912 C>T), RS1001620871 (17:56952863 C>T), RS1001673192 (17:56948515 A>G)

Disease associations

OMIM: gene MIM:600272 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST000175_3	Height	1.000000e-07

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5724767 (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
7.11	Kd	78	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	2179222: Binding affinity against COIL (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.0780	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, decreases expression	4
trichostatin A	affects expression, decreases expression	2
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
TAK-243	decreases sumoylation	1
sodium arsenite	decreases expression	1
coumarin	increases phosphorylation	1
3-deazaneplanocin	increases expression	1
ICG 001	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	affects expression, increases abundance	1
Benzo(a)pyrene	increases methylation	1
Caffeine	affects phosphorylation	1
Camptothecin	increases expression	1
Cisplatin	increases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Ethyl Methanesulfonate	increases expression	1
Formaldehyde	decreases expression	1
Ivermectin	decreases expression	1
Methyl Methanesulfonate	increases expression	1
Ozone	affects expression, increases abundance	1
Potassium Dichromate	increases expression	1
Quercetin	decreases expression	1
Ribonucleotides	affects binding	1
Rotenone	decreases expression	1
Smoke	decreases expression	1
Tretinoin	decreases expression	1
Urethane	decreases expression	1
Cyclosporine	increases expression	1
Cadmium Chloride	decreases 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
CHEMBL5697600	Binding	Inhibition of COIL (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

1 cell lines: 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1NT	Abcam HeLa COIL KO	Cancer cell line	Female

Clinical trials (associated diseases)

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