IK

Summary

IK (IK cytokine, HGNC:5958) is a protein-coding gene on chromosome 5q31.3, encoding Protein Red (Q13123). Involved in pre-mRNA splicing as a component of the spliceosome. It is a common-essential gene (DepMap: required in 99.9% of cancer cell lines).

The protein encoded by this gene was identified by its RED repeat, a stretch of repeated arginine, glutamic acid and aspartic acid residues. The protein localizes to discrete dots within the nucleus, excluding the nucleolus. Its function is unknown. This gene maps to chromosome 5; however, a pseudogene may exist on chromosome 2.

Source: NCBI Gene 3550 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 84 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 99.9% of screened cell lines (common-essential)
• MANE Select transcript: NM_006083

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:5958
Approved symbol	IK
Name	IK cytokine
Location	5q31.3
Locus type	gene with protein product
Status	Approved
Aliases	RED, RER
Ensembl gene	ENSG00000113141
Ensembl biotype	protein_coding
OMIM	600549
Entrez	3550

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 6 protein_coding, 3 retained_intron, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000417647, ENST00000502899, ENST00000503332, ENST00000507593, ENST00000508301, ENST00000512827, ENST00000513256, ENST00000515015, ENST00000515592, ENST00000523672, ENST00000947150

RefSeq mRNA: 1 — MANE Select: NM_006083 NM_006083

CCDS: CCDS47280

Canonical transcript exons

ENST00000417647 — 20 exons

Exon	Start	End
ENSE00001127945	140654516	140654586
ENSE00001127951	140653938	140654052
ENSE00001193801	140652977	140653144
ENSE00001342828	140662302	140662480
ENSE00002039967	140647829	140647924
ENSE00002434175	140660758	140660815
ENSE00002472438	140661620	140661708
ENSE00002504506	140658737	140658776
ENSE00002514209	140657554	140657662
ENSE00002528703	140658939	140659164
ENSE00002530330	140662179	140662213
ENSE00003464147	140661899	140662007
ENSE00003554155	140648471	140648537
ENSE00003565785	140652088	140652147
ENSE00003575219	140659315	140659333
ENSE00003614023	140660115	140660195
ENSE00003636273	140659756	140659834
ENSE00003688994	140651714	140651806
ENSE00003784412	140655829	140655992
ENSE00003786618	140654681	140654727

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 99.34.

FANTOM5 (CAGE): breadth broad, TPM avg 0.5624 / max 32.3279, expressed in 317 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
58924	91.5731	1824
58925	0.5624	317

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
tendon of biceps brachii	UBERON:0008188	99.34	gold quality
bronchial epithelial cell	CL:0002328	99.31	gold quality
right uterine tube	UBERON:0001302	99.27	gold quality
epithelium of bronchus	UBERON:0002031	99.14	gold quality
bronchus	UBERON:0002185	99.04	gold quality
tendon	UBERON:0000043	98.89	gold quality
sural nerve	UBERON:0015488	98.84	gold quality
calcaneal tendon	UBERON:0003701	98.79	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	98.60	gold quality
epithelium of nasopharynx	UBERON:0001951	98.29	gold quality
left testis	UBERON:0004533	98.28	gold quality
right testis	UBERON:0004534	98.24	gold quality
ganglionic eminence	UBERON:0004023	97.82	gold quality
testis	UBERON:0000473	97.80	gold quality
ventricular zone	UBERON:0003053	97.69	gold quality
type B pancreatic cell	CL:0000169	97.66	gold quality
cortical plate	UBERON:0005343	97.49	gold quality
islet of Langerhans	UBERON:0000006	97.44	gold quality
mucosa of stomach	UBERON:0001199	97.44	gold quality
mucosa of paranasal sinus	UBERON:0005030	97.40	gold quality
nasal cavity epithelium	UBERON:0005384	97.35	gold quality
popliteal artery	UBERON:0002250	97.32	gold quality
tibial artery	UBERON:0007610	97.32	gold quality
monocyte	CL:0000576	97.24	gold quality
right lung	UBERON:0002167	97.24	gold quality
descending thoracic aorta	UBERON:0002345	97.21	gold quality
leukocyte	CL:0000738	97.17	gold quality
mononuclear cell	CL:0000842	97.16	gold quality
rectum	UBERON:0001052	97.14	gold quality
gastrocnemius	UBERON:0001388	97.09	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-CURD-114	yes	60.83
E-GEOD-130148	yes	15.65
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ZBTB16

miRNA regulators (miRDB)

16 targeting IK, 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-4282	99.99	75.36	6408
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-95-5P	99.89	72.17	3973
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-3191-5P	99.24	66.52	1722
HSA-MIR-664A-3P	99.22	71.08	2696
HSA-MIR-6074	98.89	69.64	2187
HSA-MIR-6764-3P	98.44	67.64	1153
HSA-MIR-6824-3P	98.44	67.62	1154
HSA-MIR-6782-3P	97.60	67.75	931
HSA-MIR-194-3P	97.36	65.96	1027
HSA-MIR-939-5P	97.10	65.80	1579
HSA-MIR-3674	97.01	68.86	1171
HSA-MIR-1343-5P	96.48	66.06	1506
HSA-MIR-362-5P	95.87	66.02	554
HSA-MIR-500B-5P	95.87	66.04	557

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.9% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 10)

• At least three genes, orthologous to loci in this LD block, HBEGF, IK, and SRA1, result independently in a phenotype of myocardial contractile dysfunction when their expression is reduced with morpholino antisense reagents. (PMID:19064678)
• IK gene expression is decreased in follicular variant of papillary thyroid carcinoma. (PMID:21509594)
• RED is required for kinetochore localization of MAD1, mitotic progression, and activation of the spindle assembly checkpoint. (PMID:22351768)
• Data suggest that two human spliceosomal factors, RED and SMU1, are recruited to control expression and alternative splicing of viral exportins via PB2 (polymerase PB2) of influenza A virus (H3N2) and are required for efficient viral multiplication. (PMID:24945353)
• IK is an essential protein for achieving correct mitotic progress through the regulation of mitotic kinases and phosphatases (PMID:24996188)
• Data suggest an indirect radiosensitivity of hIK channels to low-dose photon irradiation with an impact on cell differentiation. (PMID:25277267)
• IK inhibits Aurora B activation through recruiting PP2A into IK and Aurora B complex. (PMID:26906715)
• Investigated and identified antiviral agents targeting the assembly of the human RED-SMU1 splicing complex, and results demonstrate possibility of RED-SMU1 destabilizing molecules to be used in antiviral therapy. (PMID:31076555)
• Smu1 and RED function both as alternative splicing regulators and as general splicing factors and are required predominantly for efficient splicing of short introns. (PMID:31409787)
• IK: A novel cell mitosis regulator that contributes to carcinogenesis. (PMID:34250629)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	ik	ENSDARG00000004161
drosophila_melanogaster	CG14722	FBGN0037943
caenorhabditis_elegans		WBGENE00012858

Paralogs (2): CSTF1 (ENSG00000101138), WDR55 (ENSG00000120314)

Protein

Protein identifiers

Protein Red — Q13123 (reviewed: Q13123)

Alternative names: Cytokine IK, IK factor, Protein RER

All UniProt accessions (6): D6RAH1, D6RAY9, D6RCQ4, D6REL4, E7EQZ7, Q13123

UniProt curated annotations — full annotation on UniProt →

Function. Involved in pre-mRNA splicing as a component of the spliceosome. Auxiliary spliceosomal protein that regulates selection of alternative splice sites in a small set of target pre-mRNA species. Required for normal mitotic cell cycle progression. Recruits MAD1L1 and MAD2L1 to kinetochores, and is required to trigger the spindle assembly checkpoint. Required for normal accumulation of SMU1. (Microbial infection) Required, together with SMU1, for normal splicing of influenza A virus NS1 pre-mRNA, which is required for the production of the exportin NS2 and for the production of influenza A virus particles. Not required for the production of VSV virus particles.

Subunit / interactions. (Microbial infection) Identified in a complex with SMU1 and influenza A virus RNA polymerase subunits PB1 and PB2. Directly interacts with SMU1 and with influenza A virus RNA polymerase subunits PB1 and PB2. Component of the spliceosome B complex. Interacts with SMU1. Interacts with MAD1L1. May interact with DHX15.

Subcellular location. Nucleus. Nucleoplasm. Chromosome. Cytoplasm. Cytoskeleton. Spindle pole.

Tissue specificity. Ubiquitous.

Induction. Up-regulated during mitosis (at protein level).

Similarity. Belongs to the RED family.

RefSeq proteins (1): NP_006074* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR012492	RED_C	Domain
IPR012916	RED_N	Domain
IPR039896	Red-like	Family

Pfam: PF07807, PF07808

UniProt features (54 total): repeat 17, cross-link 14, modified residue 7, compositionally biased region 5, region of interest 4, strand 3, sequence conflict 2, chain 1, helix 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
6Q8I	X-RAY DIFFRACTION	3.17
8QZS	ELECTRON MICROSCOPY	4.1
5O9Z	ELECTRON MICROSCOPY	4.5
8QO9	ELECTRON MICROSCOPY	5.29
9R8V	ELECTRON MICROSCOPY	8.5

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q13123-F1	68.95	0.11

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 (21): 98, 137, 287, 417, 460, 485, 536, 151, 310, 331, 386, 388, 404, 408, 496, 501, 509, 541, 543, 544 …

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-72163	mRNA Splicing - Major Pathway

MSigDB gene sets: 205 (showing top): GOBP_CHROMOSOME_ORGANIZATION, GOBP_REGULATION_OF_NUCLEAR_DIVISION, GCM_NPM1, MORF_UBE2I, GOBP_CELL_CYCLE_PHASE_TRANSITION, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, MORF_RAD21, GOBP_CHROMOSOME_SEPARATION, MORF_PSMC2, SHIPP_DLBCL_CURED_VS_FATAL_DN, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GCM_PSME1, GCM_PPP1CC, MORF_RAF1, GOBP_ORGANELLE_FISSION

GO Biological Process (6): mitotic cell cycle (GO:0000278), mRNA splicing, via spliceosome (GO:0000398), mitotic spindle assembly checkpoint signaling (GO:0007094), protein localization to kinetochore (GO:0034501), mRNA processing (GO:0006397), RNA splicing (GO:0008380)

GO Molecular Function (2): identical protein binding (GO:0042802), protein binding (GO:0005515)

GO Cellular Component (11): spindle pole (GO:0000922), nucleus (GO:0005634), nucleoplasm (GO:0005654), chromosome (GO:0005694), nuclear speck (GO:0016607), U2-type precatalytic spliceosome (GO:0071005), nuclear chromosome (GO:0000228), spliceosomal complex (GO:0005681), cytoplasm (GO:0005737), cytoskeleton (GO:0005856), mitotic spindle pole (GO:0097431)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
mRNA Splicing	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
RNA processing	2
nuclear lumen	2
intracellular membraneless organelle	2
cell cycle	1
mitotic nuclear division	1
RNA splicing, via transesterification reactions with bulged adenosine as nucleophile	1
mRNA processing	1
mitotic cell cycle	1
negative regulation of mitotic metaphase/anaphase transition	1
spindle assembly checkpoint signaling	1
mitotic spindle checkpoint signaling	1
protein localization to chromosome, centromeric region	1
protein localization to condensed chromosome	1
mRNA metabolic process	1
protein binding	1
binding	1
spindle	1
intracellular membrane-bounded organelle	1
nuclear ribonucleoprotein granule	1
U2-type spliceosomal complex	1
U1 snRNP	1
U2 snRNP	1
U4/U6 x U5 tri-snRNP complex	1
precatalytic spliceosome	1
nucleus	1
chromosome	1
nuclear protein-containing complex	1
ribonucleoprotein complex	1
intracellular anatomical structure	1
spindle pole	1
mitotic spindle	1

Protein interactions and networks

STRING

1140 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
IK	COIL	P38432	648
IK	SP100	P23497	643
IK	ATN1	P54259	581
IK	CASZ1	Q86V15	482
IK	SMU1	Q2TAY7	460
IK	CD34	P28906	421
IK	MMAA	Q8IVH4	405
IK	HIVEP3	Q5T1R4	360
IK	RBPMS	Q93062	348
IK	WDR12	Q9GZL7	339
IK	LSM4	Q9Y4Z0	326
IK	UMPS	P11172	315
IK	RABAC1	Q9UI14	311
IK	CWC22	Q9HCG8	305
IK	C9	P02748	301

IntAct

186 interactions, top by confidence:

A	B	Type	Score
SMU1	IK	psi-mi:“MI:0915”(physical association)	0.870
IK	SMU1	psi-mi:“MI:0915”(physical association)	0.870
PRPF6	SART1	psi-mi:“MI:0914”(association)	0.750
DDX6	IK	psi-mi:“MI:0915”(physical association)	0.660
RAB8B	GDI1	psi-mi:“MI:0914”(association)	0.640
DDX23	PRPF4	psi-mi:“MI:0914”(association)	0.640
IK	PRPF6	psi-mi:“MI:0915”(physical association)	0.630
EFTUD2	IK	psi-mi:“MI:0915”(physical association)	0.620
CEP70	IK	psi-mi:“MI:0915”(physical association)	0.560
IK	CEP70	psi-mi:“MI:0915”(physical association)	0.560
IK	EGLN3	psi-mi:“MI:0915”(physical association)	0.560
MBD3	IK	psi-mi:“MI:0915”(physical association)	0.560
QARS1	IK	psi-mi:“MI:0915”(physical association)	0.560
IK	DR1	psi-mi:“MI:0915”(physical association)	0.560
GTF2B	IK	psi-mi:“MI:0915”(physical association)	0.560
LMNA	IK	psi-mi:“MI:0915”(physical association)	0.560
IK	DNAJB6	psi-mi:“MI:0915”(physical association)	0.560
IK	OPTN	psi-mi:“MI:0915”(physical association)	0.560
IK	SPRED1	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (289): CEP70 (Two-hybrid), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Affinity Capture-MS), IK (Co-fractionation), IK (Co-fractionation), IK (Affinity Capture-MS), IK (Affinity Capture-MS)

ESM2 similar proteins: A0JPM9, A2AQ19, O43395, O75391, O75822, P04973, P09496, P29084, P29540, Q02614, Q0VCU8, Q13123, Q15650, Q2HJ41, Q2KIA6, Q2KJF9, Q3MHJ0, Q3UGC7, Q5BK07, Q5I0B5, Q5NVI3, Q5R5F1, Q5R8D1, Q5RAD5, Q5RE03, Q5ZJ85, Q5ZJ97, Q5ZK25, Q5ZKA4, Q66HG8, Q66JS6, Q6GMH0, Q6INR1, Q6P320, Q7SXU0, Q7SYJ9, Q7TNE3, Q8BM39, Q91WE2, Q922U1

Diamond homologs: O48713, Q13123, Q5NVI3, Q66HG8, Q9Z1M8, Q9N4U5

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 168 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
mRNA Splicing	23	22.0×	9e-23
mRNA Splicing - Minor Pathway	11	21.4×	3e-10
Processing of Capped Intron-Containing Pre-mRNA	26	18.6×	9e-24
mRNA Splicing - Major Pathway	37	17.6×	7e-34
Transport of Mature Transcript to Cytoplasm	5	16.6×	5e-04
RNA Polymerase II Transcription Termination	8	15.3×	3e-06
mRNA 3’-end processing	8	13.7×	6e-06
Transport of Mature mRNA derived from an Intron-Containing Transcript	9	11.9×	4e-06

GO biological processes:

GO term	Partners	Fold	FDR
spliceosomal snRNP assembly	8	32.1×	3e-08
negative regulation of mRNA splicing, via spliceosome	6	31.7×	5e-06
RNA splicing, via transesterification reactions	6	25.8×	1e-05
U2-type prespliceosome assembly	6	25.8×	1e-05
mRNA splicing, via spliceosome	33	20.8×	2e-31
regulation of alternative mRNA splicing, via spliceosome	10	16.8×	9e-08
mRNA transport	7	12.7×	1e-04
mRNA export from nucleus	6	12.2×	7e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	38
Likely benign	10
Benign	7

Top pathogenic / likely-pathogenic (0)

SpliceAI

2248 predictions. Top by Δscore:

Variant	Effect	Δscore
5:140647922:ATA:A	donor_gain	1.0000
5:140647923:TA:T	donor_gain	1.0000
5:140647925:G:GG	donor_gain	1.0000
5:140648467:TCAG:T	acceptor_loss	1.0000
5:140648468:CAG:C	acceptor_loss	1.0000
5:140648470:G:T	acceptor_loss	1.0000
5:140648470:GGT:G	acceptor_gain	1.0000
5:140648536:CA:C	donor_gain	1.0000
5:140648538:G:GG	donor_gain	1.0000
5:140651712:A:AG	acceptor_gain	1.0000
5:140651712:A:G	acceptor_loss	1.0000
5:140651713:G:GA	acceptor_gain	1.0000
5:140651713:GA:G	acceptor_gain	1.0000
5:140651713:GAT:G	acceptor_gain	1.0000
5:140651713:GATC:G	acceptor_gain	1.0000
5:140651713:GATCA:G	acceptor_gain	1.0000
5:140651802:CATGA:C	donor_gain	1.0000
5:140651803:ATGA:A	donor_gain	1.0000
5:140651804:TGA:T	donor_gain	1.0000
5:140651805:GA:G	donor_gain	1.0000
5:140651805:GAG:G	donor_gain	1.0000
5:140651806:AG:A	donor_loss	1.0000
5:140651807:G:GG	donor_gain	1.0000
5:140651808:T:G	donor_loss	1.0000
5:140652144:AAAGG:A	donor_loss	1.0000
5:140652146:AGGT:A	donor_loss	1.0000
5:140652147:GG:G	donor_loss	1.0000
5:140652148:GTGAA:G	donor_loss	1.0000
5:140652149:T:G	donor_loss	1.0000
5:140652154:G:GT	donor_gain	1.0000

AlphaMissense

3721 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
5:140651729:T:A	N33K	1.000
5:140651729:T:G	N33K	1.000
5:140651733:G:C	D35H	1.000
5:140651734:A:G	D35G	1.000
5:140651734:A:T	D35V	1.000
5:140651736:T:A	F36I	1.000
5:140651736:T:C	F36L	1.000
5:140651736:T:G	F36V	1.000
5:140651737:T:C	F36S	1.000
5:140651737:T:G	F36C	1.000
5:140651738:C:A	F36L	1.000
5:140651738:C:G	F36L	1.000
5:140651739:A:G	R37G	1.000
5:140651740:G:C	R37T	1.000
5:140651740:G:T	R37M	1.000
5:140651741:G:C	R37S	1.000
5:140651741:G:T	R37S	1.000
5:140651746:T:C	L39P	1.000
5:140651749:T:A	L40H	1.000
5:140651749:T:C	L40P	1.000
5:140652132:G:C	R74T	1.000
5:140652132:G:T	R74M	1.000
5:140652133:G:C	R74S	1.000
5:140652133:G:T	R74S	1.000
5:140652135:G:C	R75T	1.000
5:140652135:G:T	R75M	1.000
5:140652136:G:C	R75S	1.000
5:140652136:G:T	R75S	1.000
5:140652139:A:C	K76N	1.000
5:140652139:A:T	K76N	1.000

dbSNP variants (sampled 300 via entrez): RS1000029494 (5:140661307 C>T), RS1000065251 (5:140648011 T>G), RS1000223874 (5:140658206 G>A,C), RS1000242120 (5:140662511 C>T), RS1000314787 (5:140662272 T>C), RS1000671031 (5:140649359 C>T), RS1000829137 (5:140656918 A>G), RS1000851349 (5:140651462 T>G), RS1000877115 (5:140655372 A>T), RS1000938011 (5:140649531 A>C), RS1000961668 (5:140656135 T>C), RS1000986821 (5:140647457 G>A,C,T), RS1001122884 (5:140648360 C>A,T), RS1001156936 (5:140657205 A>C,G), RS1001198011 (5:140648654 C>A)

Disease associations

OMIM: gene MIM:600549 | 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): CHEMBL2321616 (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 3 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.13	Kd	746	nM	MOLIBRESIB
6.09	IC50	820	nM	MOLIBRESIB

PubChem BioAssay actives

2 with measured affinity, of 10 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	2179247: Binding affinity against IK (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.7460	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	2
FR900359	affects phosphorylation	1
bisphenol F	affects cotreatment, increases expression	1
TAK-243	increases sumoylation	1
triphenyl phosphate	affects expression	1
uranyl acetate	affects expression	1
bisphenol A	affects cotreatment, increases expression	1
ochratoxin A	decreases expression	1
beta-methylcholine	affects expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	increases reaction, affects binding	1
poly(propyleneimine)	decreases expression	1
abrine	decreases expression	1
Sunitinib	decreases expression	1
Arsenic Trioxide	increases expression	1
Acetaminophen	increases expression	1
Air Pollutants	increases abundance, increases expression	1
Carbamazepine	affects expression	1
Dexamethasone	affects cotreatment, increases expression	1
Diethylstilbestrol	decreases expression	1
Doxorubicin	increases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Hydrogen Peroxide	affects expression	1
Indomethacin	affects cotreatment, increases expression	1
Ivermectin	decreases expression	1
Methyl Methanesulfonate	increases expression	1
Ribonucleotides	affects binding	1
Selenium	increases expression	1
Smoke	increases expression, increases abundance	1
Tobacco Smoke Pollution	decreases expression	1

ChEMBL screening assays

9 unique, capped per target: 9 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2328092	Binding	Inhibition of IK (unknown origin)	Ion channels as therapeutic targets: a drug discovery perspective. — J Med Chem

Clinical trials (associated diseases)

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