ADCK1

Summary

ADCK1 (aarF domain containing kinase 1, HGNC:19038) is a protein-coding gene on chromosome 14q24.3, encoding AarF domain-containing protein kinase 1 (Q86TW2). Appears to be essential for maintaining mitochondrial cristae formation and mitochondrial function by acting via YME1L1 in a kinase-independent manner to regulate essential mitochondrial structural proteins OPA1 and IMMT.

Predicted to enable ATP binding activity and protein serine/threonine kinase activity. Involved in negative regulation of mitochondrial fusion and positive regulation of cristae formation. Located in mitochondrion.

Source: NCBI Gene 57143 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 111 total — 1 pathogenic, 1 likely-pathogenic
• Druggable target: yes — 17 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_020421

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19038
Approved symbol	ADCK1
Name	aarF domain containing kinase 1
Location	14q24.3
Locus type	gene with protein product
Status	Approved
Aliases	FLJ39600
Ensembl gene	ENSG00000063761
Ensembl biotype	protein_coding
OMIM	620399
Entrez	57143

Gene structure

Transcript identifiers

Ensembl transcripts: 26 — 21 protein_coding, 2 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000238561, ENST00000341211, ENST00000393639, ENST00000555217, ENST00000555333, ENST00000556048, ENST00000556560, ENST00000557501, ENST00000878179, ENST00000878180, ENST00000878181, ENST00000878182, ENST00000936815, ENST00000936816, ENST00000936817, ENST00000936818, ENST00000936819, ENST00000936820, ENST00000936821, ENST00000936822, ENST00000936823, ENST00000936824, ENST00000936825, ENST00000951873, ENST00000951874, ENST00000951875

RefSeq mRNA: 8 — MANE Select: NM_020421 NM_001142545, NM_001366485, NM_001366486, NM_001366487, NM_001366488, NM_001366489, NM_001366490, NM_020421

CCDS: CCDS45144, CCDS9869

Canonical transcript exons

ENST00000238561 — 11 exons

Exon	Start	End
ENSE00000659384	77818968	77819113
ENSE00000808502	77822435	77822518
ENSE00000808505	77899100	77899258
ENSE00001655592	77800109	77800170
ENSE00002503773	77933220	77935014
ENSE00003469553	77924457	77924606
ENSE00003498729	77907803	77907919
ENSE00003586147	77887091	77887249
ENSE00003589036	77931518	77931711
ENSE00003651069	77925764	77925961
ENSE00003690035	77859076	77859279

Expression profiles

Bgee: expression breadth ubiquitous, 243 present calls, max score 94.73.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 5.5555 / max 62.7453, expressed in 1743 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
140792	4.6679	1695
140791	0.8876	594

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
pancreatic ductal cell	CL:0002079	94.73	silver quality
apex of heart	UBERON:0002098	91.90	gold quality
upper arm skin	UBERON:0004263	89.66	silver quality
epithelial cell of pancreas	CL:0000083	87.24	silver quality
gastrocnemius	UBERON:0001388	86.78	gold quality
muscle of leg	UBERON:0001383	85.99	gold quality
left ventricle myocardium	UBERON:0006566	85.99	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	85.98	gold quality
hindlimb stylopod muscle	UBERON:0004252	85.81	gold quality
heart left ventricle	UBERON:0002084	85.39	gold quality
cardiac ventricle	UBERON:0002082	85.22	gold quality
ventral tegmental area	UBERON:0002691	85.14	gold quality
deltoid	UBERON:0001476	84.91	silver quality
granulocyte	CL:0000094	84.59	gold quality
kidney epithelium	UBERON:0004819	84.36	silver quality
endothelial cell	CL:0000115	84.32	gold quality
inferior vagus X ganglion	UBERON:0005363	84.32	gold quality
cardia of stomach	UBERON:0001162	84.29	silver quality
mucosa of transverse colon	UBERON:0004991	84.28	gold quality
right adrenal gland	UBERON:0001233	84.21	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	84.06	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.99	gold quality
right adrenal gland cortex	UBERON:0035827	83.97	gold quality
prefrontal cortex	UBERON:0000451	83.95	gold quality
tibialis anterior	UBERON:0001385	83.91	silver quality
right atrium auricular region	UBERON:0006631	83.90	gold quality
cardiac atrium	UBERON:0002081	83.88	gold quality
dorsal plus ventral thalamus	UBERON:0001897	83.84	silver quality
vena cava	UBERON:0004087	83.84	silver quality
spinal cord	UBERON:0002240	83.74	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-MTAB-6379	no	186.31
E-ANND-3	no	3.87

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

40 targeting ADCK1, 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-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-185-3P	99.95	67.01	1743
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-11181-3P	99.75	66.38	2205
HSA-MIR-1296-3P	99.72	64.04	636
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-6716-5P	99.56	68.62	1244
HSA-MIR-510-3P	99.54	70.06	2965
HSA-MIR-486-3P	99.51	66.82	1901
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-6081	99.48	66.07	1446
HSA-MIR-3612	99.45	66.02	1333
HSA-MIR-650	99.45	65.77	1309
HSA-MIR-3978	99.24	68.39	2201
HSA-MIR-122B-3P	99.21	68.90	1333
HSA-MIR-21-3P	99.21	68.95	1312
HSA-MIR-6809-5P	99.13	68.45	1223
HSA-MIR-3688-5P	99.12	69.67	1091
HSA-MIR-7160-5P	99.11	67.17	2207
HSA-MIR-4434	99.10	67.01	1984
HSA-MIR-5703	99.10	67.09	2053
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-6770-5P	98.97	66.76	1853
HSA-MIR-942-3P	98.81	69.04	876
HSA-MIR-423-5P	98.69	67.48	1522

Literature-anchored findings (GeneRIF, showing 2)

• ADCK1 activates the beta-catenin/TCF signaling pathway to promote the growth and migration of colon cancer cells. (PMID:33824271)
• ADCK1 is a potential therapeutic target of osteosarcoma. (PMID:36371387)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	adck1	ENSDARG00000062561
mus_musculus	Adck1	ENSMUSG00000021044
rattus_norvegicus	Adck1	ENSRNOG00000012685
drosophila_melanogaster	Adck1	FBGN0035039
caenorhabditis_elegans		WBGENE00008410

Paralogs (4): COQ8B (ENSG00000123815), ADCK2 (ENSG00000133597), COQ8A (ENSG00000163050), ADCK5 (ENSG00000173137)

Protein

Protein identifiers

AarF domain-containing protein kinase 1 — Q86TW2 (reviewed: Q86TW2)

All UniProt accessions (4): Q86TW2, F8W9Q8, G3V3J2, G3V426

UniProt curated annotations — full annotation on UniProt →

Function. Appears to be essential for maintaining mitochondrial cristae formation and mitochondrial function by acting via YME1L1 in a kinase-independent manner to regulate essential mitochondrial structural proteins OPA1 and IMMT. The action of this enzyme is not yet clear. It is not known if it has protein kinase activity and what type of substrate it would phosphorylate (Ser, Thr or Tyr).

Subcellular location. Mitochondrion.

Similarity. Belongs to the protein kinase superfamily. ADCK protein kinase family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q86TW2-1	1	yes
Q86TW2-2	2
Q86TW2-3	3

RefSeq proteins (8): NP_001136017, NP_001353414, NP_001353415, NP_001353416, NP_001353417, NP_001353418, NP_001353419, NP_065154* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004147	ABC1_dom	Domain
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR045307	ADCK1_dom	Domain
IPR051130	Mito_struct-func_regulator	Family

Pfam: PF03109

UniProt features (12 total): mutagenesis site 3, binding site 2, splice variant 2, transit peptide 1, chain 1, sequence conflict 1, domain 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q86TW2-F1	83.98	0.49

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 315 (proton acceptor)

Ligand- & substrate-binding residues (2): 161–169; 183

Mutagenesis-validated functional residues (3):

Position	Phenotype
315	no effect on role in maintaining mitochondrial structure and function.
164	no effect on role in maintaining mitochondrial structure and function.
183	no effect on role in maintaining mitochondrial structure and function.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 98 (showing top): GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_POSITIVE_REGULATION_OF_ORGANELLE_ORGANIZATION, GOBP_CRISTAE_FORMATION, SP1_Q2_01, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_LIPID_HOMEOSTASIS, GOBP_REGULATION_OF_MITOCHONDRION_ORGANIZATION, chr14q24, GOBP_INNER_MITOCHONDRIAL_MEMBRANE_ORGANIZATION, GOCC_MITOCHONDRIAL_ENVELOPE, GOBP_MITOCHONDRIAL_FUSION, GOBP_NEGATIVE_REGULATION_OF_DEVELOPMENTAL_PROCESS, CDPCR3HD_01, GOBP_MEMBRANE_ORGANIZATION

GO Biological Process (5): mitochondrion organization (GO:0007005), negative regulation of mitochondrial fusion (GO:0010637), lipid homeostasis (GO:0055088), positive regulation of cristae formation (GO:1903852), protein phosphorylation (GO:0006468)

GO Molecular Function (6): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (2): mitochondrion (GO:0005739), mitochondrial inner membrane (GO:0005743)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
organelle organization	1
mitochondrial fusion	1
regulation of mitochondrial fusion	1
negative regulation of organelle organization	1
negative regulation of developmental process	1
chemical homeostasis	1
positive regulation of organelle organization	1
cristae formation	1
regulation of cristae formation	1
phosphorylation	1
protein modification process	1
protein kinase activity	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
cytoplasm	1
intracellular membrane-bounded organelle	1
organelle inner membrane	1
mitochondrial membrane	1

Protein interactions and networks

STRING

1086 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ADCK1	COQ3	Q9NZJ6	619
ADCK1	COQ4	Q9Y3A0	577
ADCK1	COQ5	Q5HYK3	555
ADCK1	ADCK2	Q7Z695	530
ADCK1	COQ9	O75208	521
ADCK1	SLIRP-OT1	Q8N769	479
ADCK1	TMEM239	Q8WW34	474
ADCK1	COQ6	Q9Y2Z9	473
ADCK1	COQ2	Q96H96	451
ADCK1	PRUNE2	Q8WUY3	447
ADCK1	COQ7	Q99807	433
ADCK1	PDSS1	Q5T2R2	418
ADCK1	PPTC7	Q8NI37	401
ADCK1	CDC73	Q6P1J9	400
ADCK1	KRTAP12-2	P59991	386

IntAct

45 interactions, top by confidence:

A	B	Type	Score
PRELID1	TRIAP1	psi-mi:“MI:0914”(association)	0.730
CXCR4	TMEM120B	psi-mi:“MI:0914”(association)	0.530
SLC31A1	C2orf72	psi-mi:“MI:0914”(association)	0.530
SLC15A1	METTL15	psi-mi:“MI:0914”(association)	0.530
IL13RA2	METTL15	psi-mi:“MI:0914”(association)	0.530
APLNR	METTL15	psi-mi:“MI:0914”(association)	0.530
NPY2R	RTL8C	psi-mi:“MI:0914”(association)	0.530
PLAUR	XRCC3	psi-mi:“MI:0914”(association)	0.530
SLCO1B3	LGALS3	psi-mi:“MI:0914”(association)	0.530
ADCK1	HNRNPDL	psi-mi:“MI:0915”(physical association)	0.400
ADCK1	HMGA1	psi-mi:“MI:0915”(physical association)	0.400
EXOC5	ADCK1	psi-mi:“MI:0915”(physical association)	0.370
	TBKBP1	psi-mi:“MI:0914”(association)	0.350
ADCK1	MLYCD	psi-mi:“MI:0914”(association)	0.350
ADCK1	ALDH1L1	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
ADCK1	BCKDK	psi-mi:“MI:0914”(association)	0.350
IGHM	ESYT2	psi-mi:“MI:0914”(association)	0.350
RAMP2	GXYLT2	psi-mi:“MI:0914”(association)	0.350
GPR17	TMEM120B	psi-mi:“MI:0914”(association)	0.350
HCST	TMEM120B	psi-mi:“MI:0914”(association)	0.350
RUSF1	TMEM120B	psi-mi:“MI:0914”(association)	0.350
SV2A	ILVBL	psi-mi:“MI:0914”(association)	0.350
MLNR	NBAS	psi-mi:“MI:0914”(association)	0.350
GPR182	METTL15	psi-mi:“MI:0914”(association)	0.350
OPRL1	METTL15	psi-mi:“MI:0914”(association)	0.350
GLMP	RTL8C	psi-mi:“MI:0914”(association)	0.350
VIPR2	RABGAP1L	psi-mi:“MI:0914”(association)	0.350

BioGRID (92): ADCK1 (Affinity Capture-RNA), ADCK1 (Affinity Capture-RNA), ADCK1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), STOML2 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), TOMM5 (Affinity Capture-MS), CHCHD3 (Affinity Capture-MS), IMMT (Affinity Capture-MS), ATP5H (Affinity Capture-MS), MLYCD (Affinity Capture-MS)

ESM2 similar proteins: A0A172M468, O04212, O04226, O60111, O65361, O81852, P27697, P32296, P37142, P49079, P49080, P54887, P54888, Q02981, Q06567, Q08B22, Q0WUI9, Q10P01, Q17CS8, Q1JPL4, Q33DR2, Q39227, Q3MIX3, Q3TZM9, Q4V831, Q5M7P6, Q5ZMT7, Q6INL7, Q6K8E7, Q6P312, Q75HZ9, Q7G4P2, Q80V03, Q86TW2, Q8S948, Q941T1, Q94AX4, Q94IB8, Q96480, Q9CAP8

Diamond homologs: A0A172M468, A0KEF8, A0L1M6, A1AI24, A1RP80, A1SAK0, A1U669, A3D9F4, A3QIE3, A4STK9, A4WFY3, A4XPM5, A4Y2Q3, A5F4G3, A6WIE7, A7MQL5, A7ZU42, A8A6U2, A8ACY4, A8G8C0, A8H968, A9KYL6, B0RLZ0, B0TJ18, B0U2R2, B1IW70, B1KR05, B1LM23, B1XAJ9, B1XWR5, B2I583, B2ST34, B2TVI6, B2VG47, B3PH50, B5FF80, B5YY84, B6EHA6, B6I4H7, B7L998

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 59 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
Peptide ligand-binding receptors	7	13.0×	1e-04
G alpha (q) signalling events	6	8.6×	3e-03
G alpha (i) signalling events	7	6.8×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	5	22.8×	3e-04
phospholipase C-activating G protein-coupled receptor signaling pathway	7	19.2×	3e-05
positive regulation of cytosolic calcium ion concentration	6	14.6×	3e-04
G protein-coupled receptor signaling pathway	10	7.5×	1e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	82
Likely benign	5
Benign	0

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
686858	GRCh37/hg19 14q24.3-32.11(chr14:77274990-89803137)x1	Pathogenic
148347	GRCh38/hg38 14q24.3-31.1(chr14:77193005-80476132)x1	Likely pathogenic

SpliceAI

2815 predictions. Top by Δscore:

Variant	Effect	Δscore
14:77818964:GCA:G	acceptor_loss	1.0000
14:77818965:CAGG:C	acceptor_loss	1.0000
14:77818966:A:AG	acceptor_gain	1.0000
14:77818966:AG:A	acceptor_gain	1.0000
14:77818966:AGG:A	acceptor_loss	1.0000
14:77818967:G:GT	acceptor_gain	1.0000
14:77818967:GG:G	acceptor_gain	1.0000
14:77818967:GGA:G	acceptor_gain	1.0000
14:77818967:GGAT:G	acceptor_gain	1.0000
14:77818967:GGATC:G	acceptor_gain	1.0000
14:77819053:TAAC:T	donor_gain	1.0000
14:77819054:AACA:A	donor_gain	1.0000
14:77819055:ACAA:A	donor_gain	1.0000
14:77819059:G:GG	donor_gain	1.0000
14:77819114:G:T	donor_loss	1.0000
14:77819115:T:G	donor_loss	1.0000
14:77822425:T:TA	acceptor_gain	1.0000
14:77822429:TCACA:T	acceptor_loss	1.0000
14:77822430:CACA:C	acceptor_loss	1.0000
14:77822431:ACAGA:A	acceptor_loss	1.0000
14:77822432:CAGAC:C	acceptor_loss	1.0000
14:77822433:A:AG	acceptor_gain	1.0000
14:77822433:AGAC:A	acceptor_gain	1.0000
14:77822433:AGACG:A	acceptor_gain	1.0000
14:77822434:G:C	acceptor_loss	1.0000
14:77822434:G:GG	acceptor_gain	1.0000
14:77822434:GAC:G	acceptor_gain	1.0000
14:77822434:GACG:G	acceptor_gain	1.0000
14:77822434:GACGG:G	acceptor_gain	1.0000
14:77822515:TAAGG:T	donor_loss	1.0000

AlphaMissense

3449 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000002691 (14:77880334 GC>G), RS1000020344 (14:77896121 C>G), RS1000093064 (14:77868523 C>T), RS1000102647 (14:77810597 T>C), RS1000126955 (14:77854424 G>A), RS1000194796 (14:77859803 A>G), RS1000198423 (14:77882953 A>C), RS1000199065 (14:77898872 A>C,G), RS1000202100 (14:77818594 T>C), RS1000225832 (14:77860137 G>A), RS1000302463 (14:77934925 A>G), RS1000304306 (14:77908590 A>G), RS1000308290 (14:77824216 T>C), RS1000309366 (14:77856487 A>G), RS1000318781 (14:77889367 G>A)

Disease associations

OMIM: gene MIM:620399 | 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
GCST002366_9	Response to anti-retroviral therapy (ddI/d4T) in HIV-1 infection (Grade 1 peripheral neuropathy)	4.000000e-06
GCST003818_28	Resting heart rate	5.000000e-08
GCST004071_16	Cerebrospinal T-tau levels	8.000000e-06
GCST007208_20	Obsessive-compulsive disorder	8.000000e-07

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0000180	HIV-1 infection
EFO:0004760	t-tau measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4105885 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 54,813 (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
CHEMBL1078178	MOMELOTINIB	4	3,481
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL2103830	FOSTAMATINIB	4	3,841
CHEMBL3301607	FILGOTINIB	4	2,905
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL1236682	REFAMETINIB	2	3,223
CHEMBL1944698	ZOTIRACICLIB	2	2,915
CHEMBL1976040	ADAVOSERTIB	2	1,738
CHEMBL253969	OSI-632	2	1,150
CHEMBL475251	R-406	2	762
CHEMBL495727	AT-9283	2	1,376
CHEMBL1090479	GSK-1070916	1	177
CHEMBL3545328	XL-019	1	715
CHEMBL482967	CYC-116	1	651

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs56240334	ADCK1		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — ABC1-B subfamily

ChEMBL bioactivities

22 potent at pChembl≥5 of 24 total, top 22 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.64	Kd	23	nM	ZOTIRACICLIB
7.62	Kd	24	nM	R-406
7.48	Kd	33	nM	PACRITINIB
7.40	Kd	40	nM	ABEMACICLIB
7.24	Kd	58.09	nM	CHEMBL5653589
7.03	ED50	93.29	nM	CHEMBL5653589
6.82	Kd	152	nM	GILTERITINIB
6.70	Kd	202	nM	XL-019
6.66	Kd	217	nM	MOMELOTINIB
6.64	Kd	231	nM	FEDRATINIB
6.55	Kd	281	nM	OSI-632
6.26	Kd	545	nM	CYC-116
6.25	Kd	559	nM	AT-9283
6.11	Kd	778	nM	REFAMETINIB
5.97	Kd	1071	nM	FOSTAMATINIB
5.88	Kd	1319	nM	CHEMBL4084193
5.72	Kd	1896	nM	ADAVOSERTIB
5.69	Kd	2028	nM	FILGOTINIB
5.63	Kd	2356	nM	CHEMBL3752910
5.42	ED50	3783	nM	CHEMBL3752910
5.35	Kd	4497	nM	CHEMBL3990456
5.21	Kd	6090	nM	K-252A

PubChem BioAssay actives

21 with measured affinity, of 249 total; 21 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
(16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0230	uM
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0240	uM
Pacritinib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0330	uM
Abemaciclib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0400	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2147805: Binding affinity to human ADCK1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0581	uM
Gilteritinib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.1520	uM
N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2020	uM
Momelotinib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2170	uM
Fedratinib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2310	uM
3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-(4-pyrrolidin-1-ylbutylcarbamoylamino)-1,2-thiazole-4-carboxamide	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2810	uM
4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.5450	uM
1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.5590	uM
N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.7780	uM
Fostamatinib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.0710	uM
1-[6-(2-hydroxypropan-2-yl)-2-pyridinyl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.8960	uM
N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	2.0280	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2147805: Binding affinity to human ADCK1 incubated for 45 mins by Kinobead based pull down assay	kd	2.3555	uM
2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	4.4970	uM
methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	6.0900	uM
Pazopanib	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	16.2180	uM
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea	1424904: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	22.7470	uM

CTD chemical–gene interactions

13 total (human), top 13 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
aristolochic acid I	decreases expression	1
sodium arsenite	increases abundance, increases expression	1
zinc chromate	decreases expression, increases abundance	1
di-n-butylphosphoric acid	affects expression	1
chromium hexavalent ion	decreases expression, increases abundance	1
Air Pollutants	increases abundance, increases expression	1
Arsenic	increases abundance, increases expression	1
Doxorubicin	decreases expression	1
Hydrogen Peroxide	affects expression	1
Tobacco Smoke Pollution	decreases expression	1
Tretinoin	decreases expression	1
Valproic Acid	decreases expression	1
Particulate Matter	increases abundance, 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
CHEMBL3991617	Binding	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by ma	The target landscape of clinical kinase drugs. — Science

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_SB56	HAP1 ADCK1 (-) 1	Cancer cell line	Male
CVCL_SB57	HAP1 ADCK1 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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