CHRNA9

Summary

CHRNA9 (cholinergic receptor nicotinic alpha 9 subunit, HGNC:14079) is a protein-coding gene on chromosome 4p14, encoding Neuronal acetylcholine receptor subunit alpha-9 (Q9UGM1). Component of neuronal acetylcholine receptors (nAChRs) that function as pentameric, ligand-gated cation channels with high calcium permeability among other activities. nAChRs are excitatory neurotrasnmitter receptors formed by a collection of nAChR subunits known to mediate syna….

This gene is a member of the ligand-gated ionic channel family and nicotinic acetylcholine receptor gene superfamily. It encodes a plasma membrane protein that forms homo- or hetero-oligomeric divalent cation channels. This protein is involved in cochlea hair cell development and is also expressed in the outer hair cells (OHCs) of the adult cochlea.

Source: NCBI Gene 55584 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 80 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_017581

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14079
Approved symbol	CHRNA9
Name	cholinergic receptor nicotinic alpha 9 subunit
Location	4p14
Locus type	gene with protein product
Status	Approved
Aliases	NACHRA9
Ensembl gene	ENSG00000174343
Ensembl biotype	protein_coding
OMIM	605116
Entrez	55584

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 2 protein_coding_CDS_not_defined, 1 protein_coding

ENST00000310169, ENST00000502377, ENST00000509518

RefSeq mRNA: 1 — MANE Select: NM_017581 NM_017581

CCDS: CCDS3459

Canonical transcript exons

ENST00000310169 — 5 exons

Exon	Start	End
ENSE00001205478	40348882	40349414
ENSE00001205482	40337210	40337364
ENSE00001205488	40335827	40335972
ENSE00001205492	40353979	40355217
ENSE00001205499	40335333	40335531

Expression profiles

Bgee: expression breadth broad, 82 present calls, max score 85.70.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2359 / max 48.0290, expressed in 70 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
47437	0.1330	49
47440	0.0594	19
47439	0.0175	7
47438	0.0156	5
47436	0.0104	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	85.70	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	74.19	gold quality
penis	UBERON:0000989	68.53	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	67.66	gold quality
right uterine tube	UBERON:0001302	63.09	gold quality
tibialis anterior	UBERON:0001385	61.33	silver quality
pancreatic ductal cell	CL:0002079	59.62	silver quality
lower esophagus mucosa	UBERON:0035834	58.81	gold quality
bronchial epithelial cell	CL:0002328	58.34	silver quality
epithelium of bronchus	UBERON:0002031	57.70	silver quality
cranial nerve II	UBERON:0000941	57.33	silver quality
bronchus	UBERON:0002185	57.07	silver quality
decidua	UBERON:0002450	56.55	gold quality
mammalian vulva	UBERON:0000997	54.69	silver quality
nasal cavity mucosa	UBERON:0001826	54.29	gold quality
deltoid	UBERON:0001476	54.10	silver quality
skin of leg	UBERON:0001511	51.31	gold quality
epithelial cell of pancreas	CL:0000083	51.13	gold quality
stromal cell of endometrium	CL:0002255	49.67	gold quality
quadriceps femoris	UBERON:0001377	49.67	gold quality
fallopian tube	UBERON:0003889	49.50	gold quality
Brodmann (1909) area 46	UBERON:0006483	49.30	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
cervix squamous epithelium	UBERON:0006922	49.20	gold quality
olfactory bulb	UBERON:0002264	48.92	gold quality
choroid plexus epithelium	UBERON:0003911	48.89	gold quality
myocardium	UBERON:0002349	48.87	gold quality
type B pancreatic cell	CL:0000169	48.83	gold quality
skin of hip	UBERON:0001554	48.67	silver quality
cardiac muscle of right atrium	UBERON:0003379	48.55	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.76

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

37 targeting CHRNA9, 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-1277-5P	100.00	73.95	5056
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-659-3P	99.85	70.69	1620
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-374C-5P	99.80	72.06	2910
HSA-MIR-655-3P	99.80	72.19	2909
HSA-MIR-5700	99.64	69.88	2280
HSA-MIR-105-5P	99.54	69.24	2060
HSA-MIR-7853-5P	99.54	69.30	2055
HSA-MIR-3182	99.40	68.15	2454
HSA-MIR-6839-3P	99.39	68.86	1301
HSA-MIR-19A-5P	99.36	66.93	1675
HSA-MIR-19B-1-5P	99.36	67.07	1669
HSA-MIR-19B-2-5P	99.36	67.07	1669
HSA-MIR-1912-3P	99.32	67.40	936
HSA-MIR-3940-5P	99.14	65.26	493
HSA-MIR-4507	99.14	65.27	515
HSA-MIR-452-3P	99.01	66.25	1241
HSA-MIR-138-2-3P	98.91	68.33	1643
HSA-MIR-629-5P	98.78	68.72	1032
HSA-MIR-4780	98.57	64.75	611
HSA-MIR-216B-3P	98.55	67.19	1223
HSA-MIR-6883-3P	97.97	67.35	643
HSA-MIR-127-5P	97.78	67.64	869

Literature-anchored findings (GeneRIF, showing 18)

• Chromosome location and characterization of the CHRNA9 gene. (PMID:12697997)
• two cis-elements of the alpha9 nicotinic receptor subunit promoter control in opposite ways the basal transcriptional activity of the gene (PMID:12860975)
• Signaling through alpha9 AChR is critical for completion of the very early stages of epithelialization. (PMID:17706194)
• These results suggest that alpha9-nAChR-mediated cyclin D3 overexpression is important for nicotine-induced transformation of normal human breast epithelial cells. (PMID:20229177)
• The alpha9-nAChR is important for nicotine-induced transformation of normal human breast epithelial cells. Results imply that receptor-mediated carcinogenic signals play a decisive role in biological functions related to human breast cancer development. (PMID:20733118)
• Estrogen receptor-alpha plays a central role in mediating alpha9-nAChR gene up-regulation in response to either nicotine or estradiol stimulation. (PMID:20953833)
• Significant increases in the alpha9-nAChR mRNA and protein levels in MCF-7 cells were detected 6 h after nicotine treatment. Nicotine- and estrogen-induced alpha9-nicotinic acetylcholine receptor upregulation was blocked by (-)-epigallocatechin-3-gallate. (PMID:21370452)
• Data suggest that the biologic activities of Alpha9 nicotinic receptor (CHRNA9) may be regulated at the splicing level, and genetic polymorphisms in CHRNA9 affecting protein levels, amino acid sequence and RNA splicing may influence the risk for lung cancer. (PMID:22125646)
• Thia case-control analysis revealed that an increased risk of lung cancer is associated with two SNPs in CHRNA9, rs56159866 and rs6819385. (PMID:22280835)
• A two order of magnitude species difference in potency of alpha-conotoxin RgIA is reported for rat versus human alpha9alpha10 nAChR. (PMID:22774872)
• CHRNA9 polymorphisms are associated with non-small cell lung cancer. (PMID:24676996)
• Our findings support a significant interaction effect existing between the CHRNA9 gene and smoking exposure on the risk of breast cancer development. (PMID:25142973)
• The rare variants in CHRNA9 were significantly associated with smoking status. (PMID:25450229)
• phosphocholine inhibits ion-channel function of ATP receptor P2X7 in monocytic cells via nAChR containing alpha9 and alpha10 subunits. (PMID:27349288)
• Chemotherapy induced cold allodynia is reduced in alpha 9 knockout mice. (PMID:28223528)
• Behavioural and physiological stress-induced changes observed in alpha9-nAChR KO mice demonstrate a novel role of the alpha9alpha10-nAChR in mounting a normal stress response. The lack of functioning alpha9alpha10-nAChRs leads to negative affective changes after a relatively short period of stress. KO mice exhibited unusual patterns of circadian activity and a dysfunction in reward seeking after a period of reduced acc… (PMID:28408300)
• REVIEW: details the history and state of the field regarding the role that alpha9-containing nAChRs may play in neuropathic pain (PMID:28662295)
• Hair cell alpha9alpha10 nicotinic acetylcholine receptor functional expression regulated by ligand binding and deafness gene products. (PMID:32929005)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	chrna9a	ENSDARG00000054680
danio_rerio	chrna9b	ENSDARG00000099181
mus_musculus	Chrna9	ENSMUSG00000029205
rattus_norvegicus	Chrna9	ENSRNOG00000002484

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), CHRNA10 (ENSG00000129749), 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), CHRNA7 (ENSG00000175344), HTR3C (ENSG00000178084), GABRG3 (ENSG00000182256), GABRR3 (ENSG00000183185), HTR3E (ENSG00000186038), HTR3D (ENSG00000186090)

Protein

Protein identifiers

Neuronal acetylcholine receptor subunit alpha-9 — Q9UGM1 (reviewed: Q9UGM1)

Alternative names: Nicotinic acetylcholine receptor subunit alpha-9

All UniProt accessions (1): Q9UGM1

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 among other activities. nAChRs are excitatory neurotrasnmitter receptors formed by a collection of nAChR subunits known to mediate synaptic transmission in the nervous system and the neuromuscular junction. 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 either homopentamers or heteropentamers with CHRNA10. 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 mediate central nervous system control of auditory and vestibular sensory processing. 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 heteropentameric channels in conjunction with CHRNA10. The native outer hair cell receptor is 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 cochlea, keratinocytes, pituitary gland, B-cells and T-cells.

Post-translational modifications. N-glycosylated.

Activity regulation. Activated by a myriad of ligands such as acetylcholine. AChR activity is inhibited by the antagonist 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-9/CHRNA9 sub-subfamily.

RefSeq proteins (1): NP_060051* (*=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 (41 total): strand 13, turn 4, transmembrane region 4, sequence variant 3, mutagenesis site 3, helix 3, glycosylation site 2, disulfide bond 2, topological domain 2, binding site 2, signal peptide 1, chain 1, site 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
4UXU	X-RAY DIFFRACTION	1.71
4D01	X-RAY DIFFRACTION	1.79
6HY7	X-RAY DIFFRACTION	2.26
4UY2	X-RAY DIFFRACTION	2.7

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UGM1-F1	81.07	0.46

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): 146 (key residue important for potent inhibition of the chrna9:chrna10 receptor by the alpha-conotoxin rgia (ac p0c1d0))

Ligand- & substrate-binding residues (2): 191; 193

Disulfide bonds (2): 155–169, 219–220

Glycosylation sites (2): 57, 170

Mutagenesis-validated functional residues (3):

Position	Phenotype
86	the chrna9:chrna10 receptor is 250-fold more potently inhibited by the alpha-conotoxin rgia.
172	decreases response to acetylcholine.
228	loss of response to acetylcholine.

Function

Pathways and Gene Ontology

Reactome pathways

10 pathways

ID	Pathway
R-HSA-629594	Highly calcium permeable postsynaptic nicotinic acetylcholine receptors
R-HSA-9667769	Acetylcholine inhibits contraction of outer hair cells
R-HSA-112314	Neurotransmitter receptors and postsynaptic signal transmission
R-HSA-112315	Transmission across Chemical Synapses
R-HSA-112316	Neuronal System
R-HSA-181431	Acetylcholine binding and downstream events
R-HSA-622327	Postsynaptic nicotinic acetylcholine receptors
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: 174 (showing top): GOBP_NEGATIVE_REGULATION_OF_ERK1_AND_ERK2_CASCADE, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_SENSORY_PERCEPTION_OF_MECHANICAL_STIMULUS, GOBP_DETECTION_OF_MECHANICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION, 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, TCF4_Q5, GOBP_ANIMAL_ORGAN_MORPHOGENESIS, GOBP_EAR_DEVELOPMENT, GOBP_REACTIVE_NITROGEN_SPECIES_METABOLIC_PROCESS

GO Biological Process (18): positive regulation of cytosolic calcium ion concentration (GO:0007204), chemical synaptic transmission (GO:0007268), response to auditory stimulus (GO:0010996), monoatomic ion transmembrane transport (GO:0034220), 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), acetylcholine receptor signaling pathway (GO:0095500), monoatomic ion transport (GO:0006811), monoatomic cation transport (GO:0006812), calcium ion transport (GO:0006816), serotonin receptor signaling pathway (GO:0007210), regulation of postsynaptic membrane potential (GO:0060078), excitatory postsynaptic potential (GO:0060079), calcium ion transmembrane transport (GO:0070588), ligand-gated ion channel signaling pathway (GO:1990806)

GO Molecular Function (9): 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), protein binding (GO:0005515)

GO Cellular Component (12): plasma membrane (GO:0005886), acetylcholine-gated channel complex (GO:0005892), neuron projection (GO:0043005), synapse (GO:0045202), cholinergic synapse (GO:0098981), postsynaptic specialization membrane (GO:0099634), transmembrane transporter complex (GO:1902495), membrane (GO:0016020), 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-8 pathways:

Category	Pathways
Postsynaptic nicotinic acetylcholine receptors	1
Sensory processing of sound by outer hair cells of the cochlea	1
Transmission across Chemical Synapses	1
Neuronal System	1
Neurotransmitter receptors and postsynaptic signal transmission	1
Acetylcholine binding and downstream events	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
monoatomic ion transport	2
regulation of membrane potential	2
signal transduction	2
serotonin receptor activity	2
regulation of postsynaptic membrane potential	2
ligand-gated monoatomic ion channel activity	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
synapse	2
synaptic membrane	2
anterograde trans-synaptic signaling	1
response to mechanical stimulus	1
transmembrane transport	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
acetylcholine receptor activity	1
postsynaptic signal transduction	1
cellular response to acetylcholine	1
transport	1
metal ion transport	1
cellular response to dopamine	1
chemical synaptic transmission, postsynaptic	1
calcium ion transport	1
monoatomic cation transmembrane transport	1
extracellular ligand-gated monoatomic ion channel activity	1
excitatory postsynaptic potential	1
monoatomic cation channel activity	1
calcium ion transmembrane transporter activity	1
excitatory extracellular ligand-gated monoatomic ion channel activity	1

Protein interactions and networks

STRING

806 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CHRNA9	CHAT	P28329	792
CHRNA9	DSG3	P32926	761
CHRNA9	GRXCR2	A6NFK2	467
CHRNA9	TMEM39A	Q9NV64	466
CHRNA9	CHRNA1	P02708	459
CHRNA9	SLC30A9	Q6PML9	458
CHRNA9	CLRN2	A0PK11	458
CHRNA9	SLC30A6	Q6NXT4	455
CHRNA9	CHRNA5	P30532	434
CHRNA9	CHRND	Q07001	433
CHRNA9	SLC30A10	Q6XR72	427
CHRNA9	GTF2A1	P52655	415
CHRNA9	N4BP2	Q86UW6	407
CHRNA9	FARP2	O94887	403
CHRNA9	NQO2	P16083	403

IntAct

11 interactions, top by confidence:

A	B	Type	Score
POLR3GL	POLR3A	psi-mi:“MI:0914”(association)	0.730
CHRNA9		psi-mi:“MI:0407”(direct interaction)	0.560
CHRNA9	CHEK1	psi-mi:“MI:0914”(association)	0.530
CHRNA9	CHRNA9	psi-mi:“MI:0407”(direct interaction)	0.440
CHRNA9	TMEM120B	psi-mi:“MI:0914”(association)	0.350
ZNF785	CASK	psi-mi:“MI:0914”(association)	0.350
PCDHGC3	HRAS	psi-mi:“MI:0914”(association)	0.350
ANKRD10	DPP9	psi-mi:“MI:0914”(association)	0.350

BioGRID (153): POM121 (Affinity Capture-MS), KIAA0922 (Affinity Capture-MS), FAM76B (Affinity Capture-MS), NUFIP2 (Affinity Capture-MS), SLC30A1 (Affinity Capture-MS), SPECC1L (Affinity Capture-MS), SLC12A9 (Affinity Capture-MS), TMX2 (Affinity Capture-MS), METTL9 (Affinity Capture-MS), NETO2 (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5A (Affinity Capture-MS), C1orf43 (Affinity Capture-MS), CCPG1 (Affinity Capture-MS), POMGNT2 (Affinity Capture-MS)

ESM2 similar proteins: A8MPY1, F1R8P4, O75311, O93430, P02713, P02714, P02715, P02716, P02717, P02718, P04759, P05376, P09628, P09660, P09690, P20782, P22770, P22771, P23415, P23416, P24046, P24524, P25110, P26714, P28476, P43144, P47742, P49580, P49582, P50572, P50573, P54244, P56475, P56476, P57695, Q05941, Q07001, Q08832, Q0II76, Q24352

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

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	72
Likely benign	6
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

943 predictions. Top by Δscore:

Variant	Effect	Δscore
4:40336357:G:A	acceptor_gain	1.0000
4:40337243:T:TA	acceptor_gain	1.0000
4:40337244:G:A	acceptor_gain	1.0000
4:40337258:T:TA	acceptor_gain	1.0000
4:40349221:G:GT	donor_gain	1.0000
4:40335528:AGAG:A	donor_loss	0.9900
4:40335529:GAG:G	donor_gain	0.9900
4:40335530:AG:A	donor_loss	0.9900
4:40335531:GGTGA:G	donor_loss	0.9900
4:40335532:G:A	donor_loss	0.9900
4:40335546:ACAC:A	donor_gain	0.9900
4:40335971:TGG:T	donor_loss	0.9900
4:40335973:G:GC	donor_loss	0.9900
4:40335973:G:GG	donor_gain	0.9900
4:40335974:T:G	donor_loss	0.9900
4:40335975:GAGTA:G	donor_loss	0.9900
4:40335976:AGTAA:A	donor_loss	0.9900
4:40336356:C:CA	acceptor_gain	0.9900
4:40337254:A:G	acceptor_gain	0.9900
4:40337362:CAA:C	donor_gain	0.9900
4:40337365:G:GG	donor_gain	0.9900
4:40353973:TTCCA:T	acceptor_loss	0.9900
4:40353974:TCCAG:T	acceptor_loss	0.9900
4:40353976:CA:C	acceptor_loss	0.9900
4:40353977:A:AG	acceptor_gain	0.9900
4:40353978:G:GG	acceptor_gain	0.9900
4:40353978:GGT:G	acceptor_gain	0.9900
4:40353978:GGTA:G	acceptor_gain	0.9900
4:40353978:GGTAA:G	acceptor_gain	0.9900
4:40335544:TGAC:T	donor_gain	0.9800

AlphaMissense

3193 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
4:40337336:T:A	W113R	1.000
4:40337336:T:C	W113R	1.000
4:40349021:T:A	C169S	1.000
4:40349022:G:C	C169S	1.000
4:40349125:G:C	W203C	1.000
4:40349125:G:T	W203C	1.000
4:40337229:T:C	L77P	0.999
4:40337258:T:A	W87R	0.999
4:40337258:T:C	W87R	0.999
4:40337260:G:C	W87C	0.999
4:40337260:G:T	W87C	0.999
4:40337279:T:A	W94R	0.999
4:40337279:T:C	W94R	0.999
4:40337281:G:C	W94C	0.999
4:40337281:G:T	W94C	0.999
4:40337338:G:C	W113C	0.999
4:40337338:G:T	W113C	0.999
4:40348973:A:C	S153R	0.999
4:40348975:C:A	S153R	0.999
4:40348975:C:G	S153R	0.999
4:40348979:T:A	C155S	0.999
4:40348979:T:C	C155R	0.999
4:40348980:G:A	C155Y	0.999
4:40348980:G:C	C155S	0.999
4:40348981:T:G	C155W	0.999
4:40349000:T:C	F162L	0.999
4:40349001:T:G	F162C	0.999
4:40349002:C:A	F162L	0.999
4:40349002:C:G	F162L	0.999
4:40349003:C:T	P163S	0.999

dbSNP variants (sampled 300 via entrez): RS1000053780 (4:40353427 G>A), RS1000054751 (4:40340231 A>G), RS10001509 (4:40349860 G>A,C,T), RS1000592236 (4:40333365 T>C), RS10007267 (4:40351225 G>A,T), RS1000770079 (4:40339017 C>T), RS10008177 (4:40338824 C>T), RS10008196 (4:40338880 C>T), RS10009228 (4:40354405 A>C,G,T), RS1000964859 (4:40334515 G>A), RS1001274153 (4:40350897 T>A), RS1001299628 (4:40339075 C>T), RS1001312239 (4:40334756 G>A,C,T), RS10015231 (4:40335549 C>A,G,T), RS1001524279 (4:40334351 A>G,T)

Disease associations

OMIM: gene MIM:605116 | 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
GCST001200_4	Graves’ disease	1.000000e-13
GCST002575_4	Body mass index (change over time)	2.000000e-07
GCST007646_2	Estimated glomerular filtration rate change in renal transplantation (donor effect)	4.000000e-06

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0005937	longitudinal BMI measurement
EFO:0005199	renal transplant outcome measurement
EFO:0007892	donor genotype effect measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2109238 (PROTEIN COMPLEX), CHEMBL2184 (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)

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

Binding affinities (BindingDB)

1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CHEMBL5517963	EC50	1630 nM

ChEMBL bioactivities

137 potent at pChembl≥5 of 159 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

125 with measured affinity, of 410 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

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, increases expression	4
Nicotine	affects cotreatment, increases expression	3
(+)-JQ1 compound	decreases expression	2
Benzo(a)pyrene	affects methylation, decreases methylation, increases mutagenesis	2
Aflatoxin B1	increases expression, increases methylation	2
ethylbenzene	affects binding, decreases reaction, increases activity	1
2-methyl-4-isothiazolin-3-one	increases expression	1
trichostatin A	increases expression	1
4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone	affects cotreatment, increases expression	1
2-xylene	affects binding, decreases reaction, increases activity	1
cupric chloride	increases expression	1
3-xylene	affects binding, decreases reaction, increases activity	1
4-xylene	increases activity, affects binding, decreases reaction	1
3’-O-(4-benzoyl)benzoyladenosine 5’-triphosphate	decreases reaction, increases reaction, increases secretion	1
methyllycaconitine	affects binding, decreases activity	1
entinostat	increases expression	1
nutlin 3	affects cotreatment, increases expression	1
abrine	decreases expression	1
conotoxin alpha-RgIA, Conus regius	affects binding, decreases activity	1
Acetaminophen	increases expression	1
Acetylcholine	affects binding, decreases reaction, increases activity	1
Bungarotoxins	affects binding, decreases activity	1
Camptothecin	increases expression	1
Carbamazepine	affects expression	1
Cisplatin	increases expression	1
Dactinomycin	affects cotreatment, increases expression	1
NAD	decreases reaction, increases reaction, increases secretion	1
Smoke	increases expression	1
Tetrachlorodibenzodioxin	increases expression	1
Dronabinol	decreases expression	1

ChEMBL screening assays

105 unique, capped per target: 102 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

Clinical trials (associated diseases)

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