CHRNA10

Summary

CHRNA10 (cholinergic receptor nicotinic alpha 10 subunit, HGNC:13800) is a protein-coding gene on chromosome 11p15.4, encoding Neuronal acetylcholine receptor subunit alpha-10 (Q9GZZ6). Component of neuronal acetylcholine receptors (nAChRs) that function as pentameric, ligand-gated cation channels with high calcium permeability. nAChRs are excitatory neurotrasnmitter receptors formed by a collection of nAChR subunits.

Predicted to enable excitatory extracellular ligand-gated monoatomic ion channel activity; serotonin-gated monoatomic cation channel activity; and transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential. Acts upstream of or within positive regulation of cytosolic calcium ion concentration. Predicted to be located in membrane. Predicted to be part of transmembrane transporter complex. Predicted to be active in cholinergic synapse; neuron projection; and postsynaptic specialization membrane.

Source: NCBI Gene 57053 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 104 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_020402

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:13800
Approved symbol	CHRNA10
Name	cholinergic receptor nicotinic alpha 10 subunit
Location	11p15.4
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000129749
Ensembl biotype	protein_coding
OMIM	606372
Entrez	57053

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000250699, ENST00000493827, ENST00000526599, ENST00000534359

RefSeq mRNA: 3 — MANE Select: NM_020402 NM_001303034, NM_001303035, NM_020402

CCDS: CCDS7745

Canonical transcript exons

ENST00000250699 — 5 exons

Exon	Start	End
ENSE00000331592	3669796	3669941
ENSE00000891100	3671252	3671384
ENSE00000891101	3665587	3666564
ENSE00003538802	3669196	3669350
ENSE00003546437	3667232	3667764

Expression profiles

Bgee: expression breadth ubiquitous, 164 present calls, max score 89.47.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
gastrocnemius	UBERON:0001388	89.47	gold quality
muscle of leg	UBERON:0001383	88.24	gold quality
hindlimb stylopod muscle	UBERON:0004252	87.43	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	80.79	gold quality
muscle organ	UBERON:0001630	79.12	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	78.88	gold quality
buccal mucosa cell	CL:0002336	76.32	gold quality
granulocyte	CL:0000094	71.54	gold quality
mucosa of transverse colon	UBERON:0004991	69.73	gold quality
lower esophagus mucosa	UBERON:0035834	68.45	gold quality
blood	UBERON:0000178	67.40	gold quality
right lobe of liver	UBERON:0001114	67.39	gold quality
cerebellar hemisphere	UBERON:0002245	67.07	gold quality
cerebellar cortex	UBERON:0002129	66.95	gold quality
right hemisphere of cerebellum	UBERON:0014890	66.95	gold quality
apex of heart	UBERON:0002098	65.99	gold quality
cerebellum	UBERON:0002037	64.94	gold quality
spleen	UBERON:0002106	64.86	gold quality
right lobe of thyroid gland	UBERON:0001119	64.28	gold quality
stromal cell of endometrium	CL:0002255	63.71	gold quality
heart left ventricle	UBERON:0002084	62.98	gold quality
mucosa of stomach	UBERON:0001199	62.78	gold quality
cardiac ventricle	UBERON:0002082	62.65	gold quality
parotid gland	UBERON:0001831	62.41	gold quality
body of stomach	UBERON:0001161	62.33	gold quality
adenohypophysis	UBERON:0002196	62.26	gold quality
left uterine tube	UBERON:0001303	62.22	gold quality
left lobe of thyroid gland	UBERON:0001120	61.89	gold quality
transverse colon	UBERON:0001157	61.79	gold quality
metanephros cortex	UBERON:0010533	61.66	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	2.06

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SOX10

miRNA regulators (miRDB)

27 targeting CHRNA10, 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-6876-5P	100.00	67.68	2126
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-1299	99.77	71.24	2389
HSA-MIR-6763-5P	99.76	64.68	1767
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-4306	99.72	70.50	3630
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-875-3P	99.63	69.47	2548
HSA-MIR-6780B-3P	99.13	67.18	622
HSA-MIR-3619-5P	99.00	68.87	2308
HSA-MIR-4260	98.78	65.37	848
HSA-MIR-3611	98.76	68.76	1290
HSA-MIR-4752	98.71	68.04	833
HSA-MIR-214-3P	98.71	68.12	2128
HSA-MIR-761	98.71	68.07	2051
HSA-MIR-1227-5P	98.65	65.32	1549
HSA-MIR-6881-3P	98.04	68.24	1777
HSA-MIR-3664-3P	97.85	67.62	1452
HSA-MIR-146B-3P	97.83	65.29	782
HSA-MIR-7106-3P	97.33	65.33	644
HSA-MIR-4286	97.20	64.37	1587
HSA-MIR-8056	97.15	64.49	769
HSA-MIR-5702	96.68	68.21	958
HSA-MIR-6762-5P	96.55	64.62	972
HSA-MIR-6845-5P	96.55	64.65	969
HSA-MIR-8081	96.42	67.75	738
HSA-MIR-4524B-3P	95.52	64.12	964

Literature-anchored findings (GeneRIF, showing 3)

• CHRNA10 may have a role in “dizziness” in response to tobacco (PMID:19760673)
• A two order of magnitude species difference is reported in potency of alpha-conotoxin RgIA for rat versus human alpha9alpha10 nAChR. (PMID:22774872)
• Hair cell alpha9alpha10 nicotinic acetylcholine receptor functional expression regulated by ligand binding and deafness gene products. (PMID:32929005)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	chrna10a	ENSDARG00000011113
mus_musculus	Chrna10	ENSMUSG00000066279
rattus_norvegicus	Chrna10	ENSRNOG00000020293

Paralogs (45): GABRA3 (ENSG00000011677), GABRA1 (ENSG00000022355), CHRNA3 (ENSG00000080644), GABRP (ENSG00000094755), CHRNA4 (ENSG00000101204), GLRA2 (ENSG00000101958), GABRE (ENSG00000102287), CHRNE (ENSG00000108556), GABRA4 (ENSG00000109158), GLRB (ENSG00000109738), GABRR2 (ENSG00000111886), GABRG2 (ENSG00000113327), CHRNB4 (ENSG00000117971), CHRNA2 (ENSG00000120903), CHRND (ENSG00000135902), CHRNA1 (ENSG00000138435), GLRA3 (ENSG00000145451), GABRA6 (ENSG00000145863), GABRB2 (ENSG00000145864), GLRA1 (ENSG00000145888), GABRR1 (ENSG00000146276), CHRNB3 (ENSG00000147432), CHRNA6 (ENSG00000147434), HTR3B (ENSG00000149305), GABRA2 (ENSG00000151834), CHRNB2 (ENSG00000160716), GABRG1 (ENSG00000163285), GABRB1 (ENSG00000163288), GABRB3 (ENSG00000166206), CHRFAM7A (ENSG00000166664), HTR3A (ENSG00000166736), CHRNA5 (ENSG00000169684), CHRNB1 (ENSG00000170175), CHRNA9 (ENSG00000174343), CHRNA7 (ENSG00000175344), HTR3C (ENSG00000178084), GABRG3 (ENSG00000182256), GABRR3 (ENSG00000183185), HTR3E (ENSG00000186038), HTR3D (ENSG00000186090)

Protein

Protein identifiers

Neuronal acetylcholine receptor subunit alpha-10 — Q9GZZ6 (reviewed: Q9GZZ6)

Alternative names: Nicotinic acetylcholine receptor subunit alpha-10

All UniProt accessions (3): Q9GZZ6, E9PNT7, E9PNX2

UniProt curated annotations — full annotation on UniProt →

Function. Component of neuronal acetylcholine receptors (nAChRs) that function as pentameric, ligand-gated cation channels with high calcium permeability. nAChRs are excitatory neurotrasnmitter receptors formed by a collection of nAChR subunits. Each nAchR subunit confers differential attributes to channel properties, including activation, deactivation and desensitization kinetics, pH sensitivity, cation permeability, and binding to allosteric modulators. Forms heteropentamers with CHRNA9. Expressed in the inner ear, in sympathetic neurons and in other non-neuronal cells, such as skin keratinocytes and lymphocytes. nAChR formed by CHRNA9:CHRNA10 is involved in modulation of auditory stimuli. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, mediates synaptic transmission between efferent olivocochlear fibers and hair cells of the cochlea, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma. May also regulate keratinocyte adhesion.

Subunit / interactions. Forms homo- or heterooligomeric channels in conjunction with CHRNA10. The native outer hair cell receptor may be composed of CHRNA9:CHRNA10 heterooligomers. Found in the stoichiometric form (CHRNA9)2:(CHRNA10)3.

Subcellular location. Synaptic cell membrane. Cell membrane.

Tissue specificity. Expressed in inner-ear tissue, tonsil, immortalized B-cells, cultured T-cells and peripheral blood lymphocytes.

Activity regulation. Activated by a myriad of ligands such as acetylcholine. AChR activity is inhibited by the antagonists alpha-conotoxins RgIA and GeXXA, small disulfide-constrained peptides from cone snails.

Miscellaneous. The heterooligomeric receptor composed of CHRNA9 and CHRNA10 has an atypical pharmacological profile, binding several non-nicotinic ligands including strychnine (a glycine receptor antagonist) and atropine (a muscarinic acetylcholine receptor antagonist).

Similarity. Belongs to the ligand-gated ion channel (TC 1.A.9) family. Acetylcholine receptor (TC 1.A.9.1) subfamily. Alpha-10/CHRNA10 sub-subfamily.

RefSeq proteins (3): NP_001289963, NP_001289964, NP_065135* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002394	Nicotinic_acetylcholine_rcpt	Family
IPR006029	Neurotrans-gated_channel_TM	Domain
IPR006201	Neur_channel	Family
IPR006202	Neur_chan_lig-bd	Domain
IPR018000	Neurotransmitter_ion_chnl_CS	Conserved_site
IPR036719	Neuro-gated_channel_TM_sf	Homologous_superfamily
IPR036734	Neur_chan_lig-bd_sf	Homologous_superfamily
IPR038050	Neuro_actylchol_rec	Homologous_superfamily

Pfam: PF02931, PF02932

Catalyzed reactions (Rhea), 4 shown:

• K(+)(in) = K(+)(out) (RHEA:29463)
• Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
• Mg(2+)(in) = Mg(2+)(out) (RHEA:29827)
• Na(+)(in) = Na(+)(out) (RHEA:34963)

UniProt features (15 total): transmembrane region 4, glycosylation site 2, disulfide bond 2, topological domain 2, signal peptide 1, chain 1, sequence variant 1, mutagenesis site 1, region of interest 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9GZZ6-F1	82.93	0.51

Functional residue map

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

Disulfide bonds (2): 154–168, 218–219

Glycosylation sites (2): 56, 40

Mutagenesis-validated functional residues (1):

Position	Phenotype
31	11-fold increase in inhibition of the achr composed of subunits chrna9 and chrna10 by the conotoxin gexxa, and no change

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-9667769	Acetylcholine inhibits contraction of outer hair cells
R-HSA-9659379	Sensory processing of sound
R-HSA-9662361	Sensory processing of sound by outer hair cells of the cochlea
R-HSA-9709957	Sensory Perception

MSigDB gene sets: 121 (showing top): GOBP_NEGATIVE_REGULATION_OF_ERK1_AND_ERK2_CASCADE, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_SENSORY_PERCEPTION_OF_MECHANICAL_STIMULUS, NKX25_02, GOBP_DETECTION_OF_MECHANICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, GOBP_SYNAPTIC_TRANSMISSION_CHOLINERGIC, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_MAPK_CASCADE, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_DETECTION_OF_MECHANICAL_STIMULUS, GOBP_ANIMAL_ORGAN_MORPHOGENESIS, GOBP_EAR_DEVELOPMENT

GO Biological Process (18): positive regulation of cytosolic calcium ion concentration (GO:0007204), chemical synaptic transmission (GO:0007268), synaptic transmission, cholinergic (GO:0007271), response to auditory stimulus (GO:0010996), monoatomic ion transmembrane transport (GO:0034220), regulation of cell population proliferation (GO:0042127), regulation of membrane potential (GO:0042391), inner ear morphogenesis (GO:0042472), detection of mechanical stimulus involved in sensory perception of sound (GO:0050910), membrane depolarization (GO:0051899), negative regulation of ERK1 and ERK2 cascade (GO:0070373), monoatomic ion transport (GO:0006811), calcium ion transport (GO:0006816), serotonin receptor signaling pathway (GO:0007210), regulation of postsynaptic membrane potential (GO:0060078), excitatory postsynaptic potential (GO:0060079), regulation of biological quality (GO:0065008), calcium ion transmembrane transport (GO:0070588)

GO Molecular Function (9): signaling receptor binding (GO:0005102), excitatory extracellular ligand-gated monoatomic ion channel activity (GO:0005231), calcium channel activity (GO:0005262), acetylcholine-gated monoatomic cation-selective channel activity (GO:0022848), serotonin-gated monoatomic cation channel activity (GO:0022850), transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential (GO:1904315), transmembrane signaling receptor activity (GO:0004888), monoatomic ion channel activity (GO:0005216), extracellular ligand-gated monoatomic ion channel activity (GO:0005230)

GO Cellular Component (14): plasma membrane (GO:0005886), acetylcholine-gated channel complex (GO:0005892), membrane (GO:0016020), axon (GO:0030424), neuron projection (GO:0043005), perikaryon (GO:0043204), synapse (GO:0045202), cholinergic synapse (GO:0098981), postsynaptic specialization membrane (GO:0099634), transmembrane transporter complex (GO:1902495), cation channel complex (GO:0034703), postsynaptic membrane (GO:0045211), synaptic membrane (GO:0097060), neurotransmitter receptor complex (GO:0098878)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Sensory processing of sound by outer hair cells of the cochlea	1
Sensory Perception	1
Sensory processing of sound	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of biological quality	2
regulation of membrane potential	2
serotonin receptor activity	2
regulation of postsynaptic membrane potential	2
ligand-gated monoatomic cation channel activity	2
transmitter-gated monoatomic ion channel activity	2
monoatomic ion channel complex	2
plasma membrane signaling receptor complex	2
cellular anatomical structure	2
synapse	2
synaptic membrane	2
anterograde trans-synaptic signaling	1
chemical synaptic transmission	1
response to mechanical stimulus	1
monoatomic ion transport	1
transmembrane transport	1
cell population proliferation	1
regulation of cellular process	1
monoatomic ion transmembrane transport	1
ear morphogenesis	1
embryonic morphogenesis	1
inner ear development	1
sensory perception of sound	1
nervous system process	1
detection of mechanical stimulus involved in sensory perception	1
negative regulation of MAPK cascade	1
ERK1 and ERK2 cascade	1
regulation of ERK1 and ERK2 cascade	1
transport	1
metal ion transport	1
signal transduction	1
cellular response to dopamine	1
chemical synaptic transmission, postsynaptic	1
biological regulation	1
calcium ion transport	1
monoatomic cation transmembrane transport	1
protein binding	1
extracellular ligand-gated monoatomic ion channel activity	1
excitatory postsynaptic potential	1
monoatomic cation channel activity	1

Protein interactions and networks

STRING

648 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CHRNA10	CHAT	P28329	763
CHRNA10	MUC2	Q02817	588
CHRNA10	CTSD	P07339	548
CHRNA10	TECTB	Q96PL2	543
CHRNA10	MYO6	Q9UM54	510
CHRNA10	OTOG	Q6ZRI0	508
CHRNA10	GRXCR2	A6NFK2	490
CHRNA10	CLRN2	A0PK11	480
CHRNA10	KCNQ4	P56696	480
CHRNA10	STRC	Q7RTU9	474
CHRNA10	OTOR	Q9NRC9	447
CHRNA10	PPP1R17	O96001	443
CHRNA10	POU4F3	Q15319	436
CHRNA10	CHRNA5	P30532	431
CHRNA10	SLC26A5	P58743	431

IntAct

2 interactions, top by confidence:

A	B	Type	Score
CHRNA10	ANO6	psi-mi:“MI:0914”(association)	0.350

BioGRID (8): SIDT2 (Affinity Capture-MS), DPY19L4 (Affinity Capture-MS), MOSPD2 (Affinity Capture-MS), DNAJC18 (Affinity Capture-MS), ANO6 (Affinity Capture-MS), SYVN1 (Affinity Capture-MS), PIGU (Affinity Capture-MS), IRF2BP2 (Affinity Capture-MS)

ESM2 similar proteins: A2AIR5, A5PK45, F1PZV2, O00222, O09009, O15303, O15399, O60391, O97583, P31423, P35349, P52849, P52850, P70579, Q00961, Q01098, Q03391, Q13467, Q14833, Q14957, Q1ZZH0, Q32KH7, Q32KI9, Q32KJ8, Q3U481, Q5FYB1, Q5NCH9, Q5RDQ8, Q61088, Q62645, Q68EF4, Q6PCB7, Q863I4, Q8CHL0, Q8K078, Q8K297, Q8NBJ5, Q8TCU5, Q8VHN2, Q91ZU9

Diamond homologs: A8WQK3, O16926, O70174, P02708, P02709, P02710, P02711, P02712, P02713, P02716, P02717, P04755, P04756, P04757, P04758, P04759, P05377, P09478, P09479, P09480, P09481, P09482, P09483, P09484, P09628, P09690, P11230, P12389, P12390, P12391, P12392, P13908, P17644, P17787, P18257, P18845, P19370, P20420, P22456, P22770

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	88
Likely benign	7
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

849 predictions. Top by Δscore:

Variant	Effect	Δscore
11:3666560:CTTCC:C	acceptor_gain	1.0000
11:3669194:A:AC	donor_gain	1.0000
11:3669195:C:CC	donor_gain	1.0000
11:3669732:ACC:A	donor_gain	1.0000
11:3669733:CCC:C	donor_gain	1.0000
11:3666563:CC:C	acceptor_gain	0.9900
11:3666564:CC:C	acceptor_gain	0.9900
11:3666565:C:CC	acceptor_gain	0.9900
11:3667224:CTGCT:C	donor_loss	0.9900
11:3667226:GCTCA:G	donor_loss	0.9900
11:3667227:CT:C	donor_loss	0.9900
11:3667228:TCAC:T	donor_loss	0.9900
11:3667229:CA:C	donor_loss	0.9900
11:3667230:A:AC	donor_gain	0.9900
11:3667230:A:C	donor_loss	0.9900
11:3667231:C:CC	donor_gain	0.9900
11:3669347:CATC:C	acceptor_gain	0.9900
11:3669779:C:CT	donor_gain	0.9900
11:3669876:T:C	acceptor_gain	0.9900
11:3671243:G:C	donor_gain	0.9900
11:3666562:TCCC:T	acceptor_loss	0.9800
11:3666564:CCTGC:C	acceptor_loss	0.9800
11:3666565:C:G	acceptor_loss	0.9800
11:3666566:T:G	acceptor_loss	0.9800
11:3667231:CCG:C	donor_gain	0.9800
11:3669208:A:AC	donor_gain	0.9800
11:3669209:C:CC	donor_gain	0.9800
11:3669227:CAAGA:C	donor_gain	0.9800
11:3669348:ATCC:A	acceptor_loss	0.9800
11:3669349:TCC:T	acceptor_loss	0.9800

AlphaMissense

2870 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:3667521:C:A	W202C	0.999
11:3667521:C:G	W202C	0.999
11:3667644:G:C	F161L	0.999
11:3667644:G:T	F161L	0.999
11:3667645:A:C	F161C	0.999
11:3667646:A:G	F161L	0.999
11:3669300:C:A	W86C	0.999
11:3669300:C:G	W86C	0.999
11:3667642:G:T	P162Q	0.998
11:3669222:C:A	W112C	0.998
11:3669222:C:G	W112C	0.998
11:3669279:C:A	W93C	0.998
11:3669279:C:G	W93C	0.998
11:3669302:A:G	W86R	0.998
11:3669302:A:T	W86R	0.998
11:3667523:A:G	W202R	0.997
11:3667523:A:T	W202R	0.997
11:3667602:C:A	W175C	0.997
11:3667602:C:G	W175C	0.997
11:3667643:G:A	P162S	0.997
11:3667666:C:T	C154Y	0.997
11:3669224:A:G	W112R	0.997
11:3669224:A:T	W112R	0.997
11:3666134:G:C	S442R	0.996
11:3666134:G:T	S442R	0.996
11:3666136:T:G	S442R	0.996
11:3667624:C:T	C168Y	0.996
11:3667643:G:T	P162T	0.996
11:3667645:A:G	F161S	0.996
11:3667666:C:G	C154S	0.996

dbSNP variants (sampled 300 via entrez): RS1000262127 (11:3667972 C>A), RS1001105716 (11:3671999 A>C), RS1001123470 (11:3672868 C>T), RS1001562591 (11:3673120 G>A,T), RS1001801412 (11:3671257 G>A), RS1001896100 (11:3671540 C>A,T), RS1002127205 (11:3667526 C>A,T), RS1002504968 (11:3665884 CTCTT>C), RS1002731688 (11:3670954 C>A), RS1004120790 (11:3665328 T>C), RS1004914577 (11:3669462 A>C,G), RS1005013621 (11:3669431 T>C), RS1005711919 (11:3671704 T>A), RS1005763660 (11:3668339 T>C), RS1005933258 (11:3670679 G>A)

Disease associations

OMIM: gene MIM:606372 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST010725_20	Malaria	4.000000e-69
GCST010725_33	Malaria	2.000000e-67
GCST010725_51	Malaria	1.000000e-55

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2109238 (PROTEIN COMPLEX), CHEMBL2551 (SINGLE PROTEIN), CHEMBL4524133 (PROTEIN COMPLEX GROUP), CHEMBL4804182 (PROTEIN COMPLEX GROUP)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 125,377 (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
CHEMBL667	ACETYLCHOLINE	4	124,626
CHEMBL1257065	STILONIUM IODIDE	2	751

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2741868	CHRNA10		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: lgic — Nicotinic acetylcholine receptors (nACh)

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
RgIA4	Antagonist	8.82	pIC50
[3H]methyllycaconitine	Antagonist	8.12	pKd

ChEMBL bioactivities

120 potent at pChembl≥5 of 139 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.30	IC50	0.05	nM	CHEMBL5219936
9.59	IC50	0.26	nM	CHEMBL5219016
9.47	IC50	0.34	nM	CHEMBL5220467
9.44	IC50	0.36	nM	CHEMBL5219752
9.41	IC50	0.39	nM	CHEMBL5220455
9.40	IC50	0.4	nM	CHEMBL5220113
9.30	IC50	0.5	nM	CHEMBL5086734
9.29	IC50	0.51	nM	CHEMBL5219791
9.25	IC50	0.56	nM	CHEMBL267841
9.05	IC50	0.9	nM	CHEMBL5090753
8.89	IC50	1.3	nM	CHEMBL5219058
8.85	IC50	1.4	nM	CHEMBL5220002
8.82	IC50	1.5	nM	CHEMBL4647678
8.82	IC50	1.5	nM	CHEMBL5089881
8.82	IC50	1.5	nM	CHEMBL5184316
8.82	IC50	1.5	nM	CHEMBL5420268
8.77	IC50	1.7	nM	CHEMBL451442
8.72	IC50	1.9	nM	CHEMBL4526368
8.68	IC50	2.1	nM	CHEMBL5218653
8.54	IC50	2.9	nM	CHEMBL5073182
8.54	IC50	2.85	nM	CHEMBL5190813
8.52	IC50	3.01	nM	CHEMBL5177606
8.51	IC50	3.08	nM	CHEMBL5176101
8.49	IC50	3.2	nM	CHEMBL6102205
8.48	IC50	3.3	nM	CHEMBL6142041
8.47	IC50	3.4	nM	CHEMBL4644407
8.43	IC50	3.7	nM	CHEMBL241120
8.40	IC50	4	nM	CHEMBL5203781
8.40	IC50	4	nM	CHEMBL5220060
8.40	IC50	4	nM	CHEMBL6078731
8.40	IC50	4	nM	CHEMBL6101859
8.39	IC50	4.1	nM	CHEMBL6101859
8.38	IC50	4.2	nM	CHEMBL599735
8.32	IC50	4.8	nM	CHEMBL4293646
8.32	IC50	4.8	nM	CHEMBL268074
8.30	IC50	5	nM	CHEMBL4291079
8.30	IC50	5	nM	CHEMBL5570016
8.28	IC50	5.2	nM	CHEMBL3104241
8.27	IC50	5.4	nM	CHEMBL454767
8.24	IC50	5.74	nM	CHEMBL5195695
8.23	IC50	5.9	nM	CHEMBL4634686
8.21	IC50	6.1	nM	CHEMBL5080428
8.20	IC50	6.31	nM	CHEMBL5171118
8.18	IC50	6.6	nM	CHEMBL4285772
8.18	IC50	6.68	nM	STILONIUM IODIDE
8.11	IC50	7.8	nM	CHEMBL6171591
8.00	IC50	10	nM	STILONIUM IODIDE
8.00	IC50	9.9	nM	CHEMBL6132723
7.98	IC50	10.4	nM	CHEMBL5182114
7.96	IC50	11	nM	CHEMBL5409922

PubChem BioAssay actives

111 with measured affinity, of 377 total; 50 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
(2S)-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]-5-carbamimidamidopentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0001	uM
(2S)-5-amino-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]pentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0003	uM
(2S)-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]-5-(carbamoylamino)pentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0003	uM
(2S)-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]pentanedioic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0004	uM
(2S)-6-amino-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]hexanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0004	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0004	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40R)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1812217: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method	ic50	0.0005	uM
(2S)-2-[[(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0005	uM
1-[5-[3,5-bis[5-(3-phenylpyridin-1-ium-1-yl)pentyl]phenyl]pentyl]-3-phenylpyridin-1-ium tribromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0006	uM
(2S)-2-[[(3S)-3-[[(1R,4S,7S,13S,16R,19R,24R,27S,30S,33S,40R)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(2,2-dihydroxyethyl)-16-[(1S)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-20,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]-5-carbamimidamidopentanoic acid	1812217: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method	ic50	0.0009	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4-(3-carbamimidamidopropyl)-33-[3-(carbamoylamino)propyl]-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0013	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-33-(3-carbamimidamidopropyl)-4-[3-(carbamoylamino)propyl]-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0014	uM
(3S)-3-[[(2S,3R)-2-[[(2R)-2-[[(2R)-2-[(2-aminoacetyl)amino]-3-sulfanylpropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoyl]amino]-4-[(2S)-2-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(4-hydroxy-3-iodophenyl)-1-oxopropan-2-yl]amino]-5-(carbamoylamino)-1-oxopentan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-oxobutanoic acid	1664082: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response measured after 5 mins by two electrode voltage-clamp assay	ic50	0.0015	uM
(2S)-2-[[(1R,4R,9R,12S,15S,18S,21R,24S,27S,33S,36S)-4-[(2-aminoacetyl)amino]-12-(3-amino-3-oxopropyl)-24-(3-carbamimidamidopropyl)-18-[3-(carbamoylamino)propyl]-33-(carboxymethyl)-36-[(1R)-1-hydroxyethyl]-15-[(4-hydroxy-3-iodophenyl)methyl]-3,11,14,17,20,23,26,32,35,38-decaoxo-6,7,40,41-tetrathia-2,10,13,16,19,22,25,31,34,37-decazatricyclo[19.17.4.027,31]dotetracontane-9-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1812217: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method	ic50	0.0015	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24S,27S,30S,33S,40R)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-33-(3-carbamimidamidopropyl)-4-[3-(carbamoylamino)propyl]-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1850708: Inhibition of human nAChR alpha9alpha10 expressed in Xenopus laevis oocytes holding potential of -70 mV by voltage-clamp based electrophysiological method	ic50	0.0015	uM
(3S)-3-[[(2S,3R)-2-[[(2R)-2-[[(2R)-2-[(2-aminoacetyl)amino]-3-sulfanylpropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoyl]amino]-4-[(2S)-2-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(4-hydroxy-3-iodophenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-oxobutanoic acid	1998643: Antagonist activity at human alpha9alpha10 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by voltage-clamp based electrophysiological assay	ic50	0.0015	uM
3-phenyl-1-[5-[2,4,5-tris[5-(3-phenylpyridin-1-ium-1-yl)pent-1-ynyl]phenyl]pent-4-ynyl]pyridin-1-ium tetrabromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0017	uM
3-[(1R,6R,9S,12S,15S,21S,24S,27S,30S,33R,36S,39S,45S,48S,53R)-24-(2-amino-2-oxoethyl)-53-[[2-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[4-[4-[[6-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-[4-[1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[2-[[(1R,6R,9S,12S,15S,21S,24S,27S,30S,33R,36S,39S,45S,48S,53R)-24-(2-amino-2-oxoethyl)-6-carbamoyl-12-(2-carboxyethyl)-30,48-bis(hydroxymethyl)-21,45-bis(1H-imidazol-5-ylmethyl)-36-methyl-9-(2-methylpropyl)-8,11,14,20,23,26,29,32,35,38,44,47,50,52-tetradecaoxo-27-propan-2-yl-3,4,55,56-tetrathia-7,10,13,19,22,25,28,31,34,37,43,46,49,51-tetradecazatetracyclo[31.17.7.015,19.039,43]heptapentacontan-53-yl]amino]-2-oxoethyl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]butanoylamino]-6-oxohexyl]amino]-4-oxobutyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]acetyl]amino]-6-carbamoyl-30,48-bis(hydroxymethyl)-21,45-bis(1H-imidazol-5-ylmethyl)-36-methyl-9-(2-methylpropyl)-8,11,14,20,23,26,29,32,35,38,44,47,50,52-tetradecaoxo-27-propan-2-yl-3,4,55,56-tetrathia-7,10,13,19,22,25,28,31,34,37,43,46,49,51-tetradecazatetracyclo[31.17.7.015,19.039,43]heptapentacontan-12-yl]propanoic acid	1561126: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-evoked currents by two-electrode voltage clamp assay	ic50	0.0019	uM
(2R)-2-[[(2R)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0021	uM
(2S)-2-[3-[[(1R,4S,7S,13S,16R,19R,24R,27S,30S,33S,40R)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-4,33-bis[3-(diaminomethylideneamino)propyl]-13-(2,2-dihydroxyethyl)-16-[(1S)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-20,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]propanoylamino]-5-(diaminomethylideneamino)pentanoic acid	1812217: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method	ic50	0.0029	uM
1-methyl-1-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]pyrrolidin-1-ium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0029	uM
1-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]-1-azoniabicyclo[2.2.2]octane iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0030	uM
1-methyl-1-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]piperidin-1-ium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0031	uM
(1R,4S,7S,13S,16S,19R,22S,25S,28S,31R,34S,37R,46S,52R)-46-amino-28-(3-amino-3-oxopropyl)-16,22-bis(3-carbamimidamidopropyl)-7-(carboxymethyl)-4-[(1R)-1-hydroxyethyl]-25-[(4-hydroxy-3-iodophenyl)methyl]-34-[(4-hydroxyphenyl)methyl]-2,5,8,14,17,20,23,26,29,32,35,43,47,50,53-pentadecaoxo-56,57,60,61-tetrathia-3,6,9,15,18,21,24,27,30,33,36,42,48,51,54-pentadecazatetracyclo[29.23.4.419,52.09,13]dohexacontane-37-carboxylic acid	1664082: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response measured after 5 mins by two electrode voltage-clamp assay	ic50	0.0034	uM
2-[5-[3,5-bis(5-isoquinolin-2-ium-2-ylpentyl)phenyl]pentyl]isoquinolin-2-ium tribromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0037	uM
2-[(1R,6R,9S,12S,15S,21S,24S,27S,30S,33R,36S,39S,45S,53R)-53-[(2-aminoacetyl)amino]-48-(aminomethyl)-21,24-bis(2-amino-2-oxoethyl)-9-[(2S)-butan-2-yl]-6-carbamoyl-30-(hydroxymethyl)-45-(1H-imidazol-5-ylmethyl)-36-methyl-8,11,14,20,23,26,29,32,35,38,44,47,50,52-tetradecaoxo-27-propan-2-yl-3,4,55,56-tetrathia-7,10,13,19,22,25,28,31,34,37,43,46,49,51-tetradecazatetracyclo[31.17.7.015,19.039,43]heptapentacontan-12-yl]acetic acid	1896181: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-induced current amplitude at -80 mV holding potential by two-electrode voltage clamp method	ic50	0.0040	uM
(2R)-2-[[(3S)-3-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-aminopropyl)-4,33-bis(3-carbamimidamidopropyl)-13-(carboxymethyl)-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-20,20-dimethyl-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-4-(4-hydroxyphenyl)butanoyl]amino]-5-carbamimidamidopentanoic acid	1916327: Inhibition of human alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response at -70 mV holding potential and measured for 1 to 5 days in presence of Ach stimulation by voltage-clamp based electrophysiological method	ic50	0.0040	uM
1-[3-[4-[4-[3-(3,4-dimethylpyridin-1-ium-1-yl)propyl]phenyl]phenyl]propyl]-3,4-dimethylpyridin-1-ium dibromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0042	uM
triethyl-[6-[4-[(E)-2-phenylethenyl]phenoxy]hexyl]azanium iodide	1418933: Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method	ic50	0.0048	uM
1-[5-[3,5-bis(5-quinolin-1-ium-1-ylpentyl)phenyl]pentyl]quinolin-1-ium tribromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0048	uM
triethyl-[4-[4-[(E)-2-phenylethenyl]phenoxy]butyl]azanium iodide	1418933: Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method	ic50	0.0050	uM
(3S)-4-amino-3-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoic acid	2098825: Antagonist activity at human wild type alpha9alpha10 nAChR expressed in acetylcholine-induced Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current at 1:3 ratio of protein by two electrode voltage-clamp assay	ic50	0.0050	uM
2-[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40R)-40-[(2-aminoacetyl)amino]-24-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]-4,27,33-tris[3-(diaminomethylideneamino)propyl]-16-(hydroxymethyl)-30-[(4-hydroxyphenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-21,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontan-13-yl]acetic acid	1062433: Inhibition of alpha9alpha10 (unknown origin) nAChR	ic50	0.0052	uM
3-phenyl-1-[5-[2,4,5-tris[5-(3-phenylpyridin-1-ium-1-yl)pentyl]phenyl]pentyl]pyridin-1-ium tetrabromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0054	uM
cyclohexyl-dimethyl-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]azanium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0057	uM
(1R,4S,7S,13S,16S,19R,22S,25S,28S,31R,34S,37R,46S,52R)-46-amino-28-(3-amino-3-oxopropyl)-16-(3-carbamimidamidopropyl)-22-[3-(carbamoylamino)propyl]-7-(carboxymethyl)-4-[(1R)-1-hydroxyethyl]-25-[(4-hydroxy-3-iodophenyl)methyl]-34-[(4-hydroxyphenyl)methyl]-2,5,8,14,17,20,23,26,29,32,35,43,47,50,53-pentadecaoxo-56,57,60,61-tetrathia-3,6,9,15,18,21,24,27,30,33,36,42,48,51,54-pentadecazatetracyclo[29.23.4.419,52.09,13]dohexacontane-37-carboxylic acid	1664082: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response measured after 5 mins by two electrode voltage-clamp assay	ic50	0.0059	uM
(2S)-2-[[(1R,4S,7S,13S,16S,19R,24R,27S,30S,33S,40S)-40-[(2-aminoacetyl)amino]-27-(3-amino-3-oxopropyl)-33-[3-(carbamoylamino)propyl]-13-(carboxymethyl)-4-[3-(diaminomethylideneamino)propyl]-16-[(1R)-1-hydroxyethyl]-30-[(4-hydroxy-3-iodophenyl)methyl]-3,6,12,15,18,26,29,32,35,41-decaoxo-20,22,37,38-tetrathia-2,5,11,14,17,25,28,31,34,42-decazatricyclo[17.16.7.07,11]dotetracontane-24-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid	1812217: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method	ic50	0.0061	uM
1,1-dimethyl-4-[4-[(E)-2-phenylethenyl]phenoxy]piperidin-1-ium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0063	uM
triethyl-[8-[4-[(E)-2-phenylethenyl]phenoxy]octyl]azanium iodide	1418933: Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method	ic50	0.0066	uM
triethyl-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]azanium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0067	uM
1-methyl-3-[4-[(E)-2-phenylethenyl]phenoxy]-1-azoniabicyclo[2.2.2]octane iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0104	uM
(2S)-2-[[(1R,4S,7S,10S,13S,16S,19S,22R,27R,30S,33S,36S,42S,45S,48R,51S,54S,60S,63S,66S,69S,72S,75S,78S,81S)-27-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-4,7,30,42,51,69,72,75,78-nonakis(3-carbamimidamidopropyl)-16,66-bis(carboxymethyl)-13-[(1R)-1-hydroxyethyl]-33,36,54-tris(hydroxymethyl)-45,63,81-tris[(4-hydroxyphenyl)methyl]-10,19-dimethyl-2,5,8,11,14,17,20,28,31,34,37,40,43,46,49,52,55,61,64,67,70,73,76,79,82-pentacosaoxo-24,25,85,86-tetrathia-3,6,9,12,15,18,21,29,32,35,38,41,44,47,50,53,56,62,65,68,71,74,77,80,83-pentacosazatricyclo[46.35.4.056,60]heptaoctacontane-22-carbonyl]amino]-3-methylbutanoic acid	1998643: Antagonist activity at human alpha9alpha10 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by voltage-clamp based electrophysiological assay	ic50	0.0110	uM
4-[4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenoxy]butyl-triethylazanium iodide	1418933: Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method	ic50	0.0119	uM
(1R,4S,7S,13S,16S,19R,22S,25S,28S,31R,34S,37R,46S,52R)-46-amino-28-(3-amino-3-oxopropyl)-16-(3-carbamimidamidopropyl)-22-[3-(carbamoylamino)propyl]-7-(carboxymethyl)-4-[(1R)-1-hydroxyethyl]-25,34-bis[(4-hydroxyphenyl)methyl]-2,5,8,14,17,20,23,26,29,32,35,43,47,50,53-pentadecaoxo-56,57,60,61-tetrathia-3,6,9,15,18,21,24,27,30,33,36,42,48,51,54-pentadecazatetracyclo[29.23.4.419,52.09,13]dohexacontane-37-carboxylic acid	1664082: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response measured after 5 mins by two electrode voltage-clamp assay	ic50	0.0152	uM
1-[3-[4-[4-[3-(3,4-dimethylpyridin-1-ium-1-yl)prop-1-ynyl]phenyl]phenyl]prop-2-ynyl]-3,4-dimethylpyridin-1-ium dibromide	590739: Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current by voltage clamp electrophysiology assay	ic50	0.0160	uM
2-[4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenoxy]ethyl-triethylazanium iodide	1418933: Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method	ic50	0.0172	uM
1,1-dimethyl-3-[4-[(E)-2-phenylethenyl]phenoxy]piperidin-1-ium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0173	uM
1-methyl-1-[2-[4-[(E)-2-phenylethenyl]phenoxy]ethyl]azetidin-1-ium iodide	1881223: Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay	ic50	0.0179	uM
(2S)-2-[[(4R,7S,10S,13S,16S,19S,22S,25R)-25-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(4R,7S,10S,16S,19S,22S,25R)-25-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-10,22-bis(3-carbamimidamidopropyl)-16,19-bis(hydroxymethyl)-7-[(4-hydroxyphenyl)methyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-16-[(2S)-butan-2-yl]-19,22-bis(3-carbamimidamidopropyl)-10-(carboxymethyl)-13-[(1R)-1-hydroxyethyl]-7-methyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carbonyl]amino]-3-methylbutanoic acid	1998643: Antagonist activity at human alpha9alpha10 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by voltage-clamp based electrophysiological assay	ic50	0.0203	uM
3-[(1R,6R,9S,12S,15S,21S,24S,27S,30S,33R,36S,39S,45S,48S,53R)-53-[(2-aminoacetyl)amino]-24-(2-amino-2-oxoethyl)-6-carbamoyl-30,48-bis(hydroxymethyl)-21,45-bis(1H-imidazol-5-ylmethyl)-36-methyl-9-(2-methylpropyl)-8,11,14,20,23,26,29,32,35,38,44,47,50,52-tetradecaoxo-27-propan-2-yl-3,4,55,56-tetrathia-7,10,13,19,22,25,28,31,34,37,43,46,49,51-tetradecazatetracyclo[31.17.7.015,19.039,43]heptapentacontan-12-yl]propanoic acid	1561126: Inhibition of human alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of ACh-evoked currents by two-electrode voltage clamp assay	ic50	0.0219	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
aristolochic acid I	increases expression	1
sotorasib	affects cotreatment, increases expression	1
ethylbenzene	affects binding, decreases reaction, increases activity	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
2-xylene	affects binding, decreases reaction, increases activity	1
3-xylene	affects binding, decreases reaction, increases activity	1
4-xylene	affects binding, decreases reaction, increases activity	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
conotoxin alpha-RgIA, Conus regius	affects binding, decreases activity	1
jinfukang	decreases expression, affects cotreatment	1
trametinib	affects cotreatment, increases expression	1
NVP-BKM120	affects cotreatment, increases expression	1
Acetaminophen	increases expression	1
Acetylcholine	affects binding, decreases reaction, increases activity	1
Air Pollutants	affects expression, increases abundance	1
Benzene	increases expression	1
Benzo(a)pyrene	increases methylation	1
Cisplatin	affects cotreatment, decreases expression	1
Ozone	affects expression, increases abundance	1
Phthalic Acids	increases methylation	1
Potassium Chloride	decreases response to substance, increases expression	1
Quercetin	increases expression	1
Silicon Dioxide	increases expression	1
Smoke	decreases expression	1
Dronabinol	decreases response to substance, increases expression	1
Tobacco Smoke Pollution	increases expression	1
Aflatoxin B1	increases methylation	1
S-Nitrosoglutathione	increases expression	1
Particulate Matter	decreases expression	1

ChEMBL screening assays

92 unique, capped per target: 89 binding, 2 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1763990	Functional	Antagonist activity at alpha9/alpha10 nAChR expressed in Xenopus oocyte assessed as inhibition of ACh-gated current response at 100 nM by voltage clamp electrophysiology assay	Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain. — Bioorg Med Chem Lett
CHEMBL2427311	Binding	Inhibition of nicotinic acetylcholine receptor subunit alpha-9 alpha-10 (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current at 3 uM by two-electrode voltage clamp method	Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists. — J Med Chem
CHEMBL4810209	ADMET	Inhibition of neuronal nicotinic receptor (unknown origin) at 0.1 to 1 uM	Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_YA34	IDG-HEK293T-CHRNA10-V5-OE	Transformed cell line	Female

Clinical trials (associated diseases)

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