GABRG1

Summary

GABRG1 (gamma-aminobutyric acid type A receptor subunit gamma1, HGNC:4086) is a protein-coding gene on chromosome 4p12, encoding Gamma-aminobutyric acid receptor subunit gamma-1 (Q8N1C3). Gamma subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain.

The protein encoded by this gene belongs to the ligand-gated ionic channel family. It is an integral membrane protein and plays an important role in inhibiting neurotransmission by binding to the benzodiazepine receptor and opening an integral chloride channel. This gene is clustered with three other family members on chromosome 4.

Source: NCBI Gene 2565 — RefSeq curated summary.

At a glance

• Gene–disease (curated): genetic developmental and epileptic encephalopathy (Limited, GenCC)
• GWAS associations: 6
• Clinical variants (ClinVar): 65 total
• GTEx eGene: eQTL in 4 tissues, sQTL in 1 (q < 0.05)
• ChEMBL bioactivity: 15 clinical-phase molecules tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.31 (unconstrained)
• MANE Select transcript: NM_173536
• Notable: 65 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4086
Approved symbol	GABRG1
Name	gamma-aminobutyric acid type A receptor subunit gamma1
Location	4p12
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000163285
Ensembl biotype	protein_coding
OMIM	137166
Entrez	2565

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

MANE Select: ENST00000295452

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1

ENST00000295452, ENST00000964875, ENST00001135362

RefSeq mRNA: 1 — MANE Select: NM_173536 NM_173536

CCDS: CCDS3470

Canonical transcript exons

ENST00000295452 — 9 exons

Exon	Start	End
ENSE00001073015	46065364	46065584
ENSE00001073017	46058485	46058622
ENSE00001073019	46097201	46097349
ENSE00001073021	46123810	46124054
ENSE00001073022	46051424	46051638
ENSE00001073024	46064441	46064523
ENSE00001073026	46083986	46084053
ENSE00001073028	46058217	46058369
ENSE00001258742	46035769	46041254

Expression profiles

Bgee: expression breadth broad, 88 present calls, max score 92.57.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 5.8550 / max 645.9126, expressed in 109 samples.

Highest expression (Bgee): medial globus pallidus, globus pallidus, endothelial cell, lateral globus pallidus, Brodmann (1909) area 23.

Genetic regulation across tissues (GTEx eQTL / sQTL)

GABRG1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 4 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

5 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Nerve Tibial	eqtl	1.1e-13	-0.29	4:46258570:T:C
Pituitary	eqtl	7.4e-03	+0.23	4:46053606:G:T
Brain Cortex	sqtl	1.9e-02	-2.41	4:46296655:G:GAA
Adipose Subcutaneous	eqtl	4.1e-02	-0.40	4:46083352:T:A
Uterus	eqtl	4.8e-02	+0.50	4:46445563:C:T

FANTOM5 promoters

4 alternative TSS:

Promoter ID	TPM avg	Samples expressed
51995	3.7866	108
51997	1.5585	94
51998	0.3200	85
51996	0.1899	77

Top tissues by expression

showing 100 of 226 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
medial globus pallidus	UBERON:0002477	92.57	gold quality
globus pallidus	UBERON:0001875	91.95	gold quality
endothelial cell	CL:0000115	90.50	gold quality
lateral globus pallidus	UBERON:0002476	89.74	gold quality
Brodmann (1909) area 23	UBERON:0013554	89.28	gold quality
entorhinal cortex	UBERON:0002728	88.74	gold quality
caudate nucleus	UBERON:0001873	88.21	gold quality
nucleus accumbens	UBERON:0001882	87.96	gold quality
temporal lobe	UBERON:0001871	86.92	gold quality
amygdala	UBERON:0001876	86.65	gold quality
Brodmann (1909) area 46	UBERON:0006483	86.38	gold quality
hypothalamus	UBERON:0001898	86.20	gold quality
superior frontal gyrus	UBERON:0002661	86.18	gold quality
postcentral gyrus	UBERON:0002581	85.89	gold quality
putamen	UBERON:0001874	85.37	gold quality
superior vestibular nucleus	UBERON:0007227	85.29	gold quality
primary visual cortex	UBERON:0002436	84.63	gold quality
Ammon’s horn	UBERON:0001954	84.48	gold quality
parietal lobe	UBERON:0001872	84.37	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	83.65	gold quality
Brodmann (1909) area 9	UBERON:0013540	83.46	gold quality
occipital lobe	UBERON:0002021	83.44	gold quality
right frontal lobe	UBERON:0002810	83.11	gold quality
anterior cingulate cortex	UBERON:0009835	83.05	gold quality
cerebral cortex	UBERON:0000956	82.98	gold quality
substantia nigra pars reticulata	UBERON:0001966	82.90	gold quality
substantia nigra	UBERON:0002038	82.84	gold quality
corpus callosum	UBERON:0002336	82.73	gold quality
medulla oblongata	UBERON:0001896	82.61	gold quality
frontal cortex	UBERON:0001870	82.27	gold quality
frontal lobe	UBERON:0016525	82.27	gold quality
neocortex	UBERON:0001950	82.23	gold quality
middle temporal gyrus	UBERON:0002771	82.18	gold quality
midbrain	UBERON:0001891	82.17	gold quality
forebrain	UBERON:0001890	81.59	gold quality
subthalamic nucleus	UBERON:0001906	80.70	gold quality
prefrontal cortex	UBERON:0000451	80.60	gold quality
brain	UBERON:0000955	80.39	gold quality
germinal epithelium of ovary	UBERON:0001304	79.98	gold quality
ventral tegmental area	UBERON:0002691	79.84	gold quality
substantia nigra pars compacta	UBERON:0001965	79.68	gold quality
dorsal plus ventral thalamus	UBERON:0001897	78.98	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.48	gold quality
inferior vagus X ganglion	UBERON:0005363	77.47	gold quality
cerebellar vermis	UBERON:0004720	77.27	gold quality
spinal cord	UBERON:0002240	73.22	gold quality
right hemisphere of cerebellum	UBERON:0014890	73.16	gold quality
cortical plate	UBERON:0005343	72.66	gold quality
lateral nuclear group of thalamus	UBERON:0002736	72.65	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	72.08	gold quality
cerebellum	UBERON:0002037	71.59	gold quality
cerebellar cortex	UBERON:0002129	71.36	gold quality
cerebellar hemisphere	UBERON:0002245	71.26	gold quality
ventricular zone	UBERON:0003053	70.11	gold quality
epithelial cell of pancreas	CL:0000083	67.32	gold quality
pons	UBERON:0000988	67.01	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	65.02	gold quality
pancreatic ductal cell	CL:0002079	60.93	silver quality
ganglionic eminence	UBERON:0004023	60.04	gold quality
nasal cavity epithelium	UBERON:0005384	59.93	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	59.22	gold quality
tibialis anterior	UBERON:0001385	58.53	silver quality
ileal mucosa	UBERON:0000331	57.89	gold quality
ovary	UBERON:0000992	56.99	gold quality
caput epididymis	UBERON:0004358	56.54	gold quality
pericardium	UBERON:0002407	55.73	gold quality
cardiac muscle of right atrium	UBERON:0003379	55.54	gold quality
vena cava	UBERON:0004087	54.91	gold quality
body of tongue	UBERON:0011876	54.76	gold quality
tongue	UBERON:0001723	54.58	gold quality
superior surface of tongue	UBERON:0007371	54.51	gold quality
left ventricle myocardium	UBERON:0006566	54.23	gold quality
kidney epithelium	UBERON:0004819	53.93	gold quality
upper leg skin	UBERON:0004262	53.52	gold quality
upper arm skin	UBERON:0004263	53.52	gold quality
quadriceps femoris	UBERON:0001377	53.37	gold quality
dorsal root ganglion	UBERON:0000044	53.06	silver quality
jejunal mucosa	UBERON:0000399	52.92	silver quality
left ovary	UBERON:0002119	52.88	gold quality
layer of synovial tissue	UBERON:0007616	51.68	gold quality
jejunum	UBERON:0002115	51.62	silver quality
adult organism	UBERON:0007023	51.49	silver quality
vastus lateralis	UBERON:0001379	51.18	gold quality
right ovary	UBERON:0002118	51.12	gold quality
oocyte	CL:0000023	50.86	gold quality
myocardium	UBERON:0002349	50.76	gold quality
saphenous vein	UBERON:0007318	50.47	gold quality
pituitary gland	UBERON:0000007	50.15	gold quality
buccal mucosa cell	CL:0002336	50.06	silver quality
tendon of biceps brachii	UBERON:0008188	49.93	gold quality
colonic epithelium	UBERON:0000397	49.03	gold quality
tibial nerve	UBERON:0001323	48.55	gold quality
trigeminal ganglion	UBERON:0001675	47.53	gold quality
nipple	UBERON:0002030	47.53	gold quality
penis	UBERON:0000989	47.40	gold quality
adenohypophysis	UBERON:0002196	47.32	gold quality
pharyngeal mucosa	UBERON:0000355	46.49	gold quality
skin of hip	UBERON:0001554	46.13	gold quality
sural nerve	UBERON:0015488	45.22	gold quality
synovial joint	UBERON:0002217	44.99	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.71

HPA expression

RNA tissue specificity: Tissue enriched

44 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Hypothalamus	tissue	109.5
Thalamus	tissue	94.1
Hippocampal formation	tissue	92.4
Midbrain	tissue	89.8
Pons	tissue	86.7
Periaqueductal gray	tissue	85.3
Septum	tissue	82.0
Amygdala	tissue	77.1
Medulla oblongata	tissue	71.5
Spinal cord	tissue	68.6
Substantia nigra	tissue	64.8
Superior colliculi	tissue	63.0
Ventral forebrain	tissue	52.2
Putamen	tissue	48.5
Entorhinal cortex	tissue	47.2
Prefrontal cortex	tissue	46.2
Cerebral cortex	tissue	46.2	medium
Motor cortex	tissue	44.9
Temporal cortex	tissue	44.1
Insular cortex	tissue	43.1
Retrosplenial cortex	tissue	42.6
Retrosplenial and cingulate cortex	tissue	42.4
Basal ganglia	tissue	40.8	medium
Occipital cortex	tissue	38.7
Cerebellum	tissue	36.2	medium
Somatosensory cortex	tissue	36.1
Corpus callosum	tissue	31.5
Nucleus accumbens	tissue	27.8
Hippocampus	tissue	25.4	low
Locus coeruleus	tissue	23.8
Olfactory bulb	tissue	21.4
Caudate putamen	tissue	21.4
Frontal cortex	tissue	19.9
Postcentral gyrus	tissue	18.3
Choroid plexus	tissue	4.5
Retina	tissue	2.7
Ovary	tissue	1.1	not detected
Pituitary gland	tissue	0.5
Testis	tissue	0.2	not detected
Fallopian tube	tissue	0.2	not detected
Adipose tissue	tissue	0.1	not detected
Thyroid gland	tissue	0.1	not detected
Spleen	tissue	0.1	not detected
Soft tissue 1	tissue	-1.0	low

Brain sub-regions (HPA Brain Atlas): detected in 188; highest nTPM — Subiculum (92.4), Ventromedial nucleus (78.6), Ventral spinal cord (68.6), Periaquaductal grey, anterior (68.2), Ventral hippocampus (55.0).

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

Targeting GABRG1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 229 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-5692A	100.00	74.40	6850
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3064-3P	100.00	70.09	1254
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-4776-3P	100.00	68.73	1340
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-1185-1-3P	99.98	71.04	2593

Functional genomics

gnomAD constraint: pLI 2.06e-12, LOEUF 1.31, missense Z 0.225 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000295452 — one region, missense o/e 1.00.

Literature-anchored findings (GeneRIF, showing 11)

• Logistic regression analysis indicated that genetic elements in the GABRG1 haplotype block likely contribute to alcohol dependence risk in an additive manner. (PMID:17507911)
• study of patterns of htSNPs & linkage disequilibrium (LD)in 6 populations; LD extended from most of the GABRA2 gene through the GABRG1 locus in the same GABAA cluster region suggesting possible association of these genes with alcohol dependence (PMID:17976953)
• results of the present study suggest that hippocampal neurons expressing GABAAgamma receptor subunits resist the progression of neurofibrillary degeneration in Alzheimer disease hippocampus (PMID:19019179)
• A single nucleotide polymorphism of the GABRG1 gene (rs1497571) is associated with level of response to alcohol and drinking patterns. (PMID:19426171)
• An intronic single nucleotide polymorphism (SNP) (rs17536211) in GABRG1 shows the strongest statistical evidence of association of recovery from eating disorders. (PMID:21750581)
• we genotyped 13 single nucleotide polymorphisms spanning GABRG1 and GABRA2 in African Americans with alcohol dependence (PMID:21919924)
• A significant GABRG1 genotype influences self-administration of alcohol and GABAergic manipulation. (PMID:22817768)
• Switching the intracellular domains of the gamma2 and gamma1 subunits substantiated this inference. Because this region determines post-synaptic localization, we hypothesize that GABAARs containing gamma1 and gamma2 use different mechanisms for synaptic clustering. (PMID:24425869)
• rs1497577 not significantly associated with adaptation to subjective responses to alcohol (PMID:26087834)
• Steady-state activation of the high-affinity isoform of the alpha4beta2delta GABAA receptor. (PMID:31690811)
• The strongest association for alcohol use disorder (rs3756007) was located in GABRA2, the strongest association for antisocial behavior (rs11941860) was located in GABRG1, and the interaction term yielded top associations in GABRA2 (rs2119183) and the intergenic region between GABRA2 and GABRG1 (rs536599). (PMID:31790348)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	gabrg1	ENSDARG00000101995
mus_musculus	Gabrg1	ENSMUSG00000001260
rattus_norvegicus	Gabrg1	ENSRNOG00000002360

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), 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), GABRA5 (ENSG00000186297), ZACN (ENSG00000186919), GABRD (ENSG00000187730), CHRNG (ENSG00000196811), GABRQ (ENSG00000268089)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:103156) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 15 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal heart morphology	1
abnormal cranium morphology	1
abnormal liver morphology	1
abnormal spleen morphology	1
small spleen	1
abnormal uterus morphology	1
abnormal lens morphology	1
abnormal cornea morphology	1
abnormal eye morphology	1
abnormal tail morphology	1
increased mean corpuscular hemoglobin concentration	1
abnormal tooth color	1
abnormal nocifensive behavior	1
increased freezing behavior	1
decreased mechanical nociceptive threshold	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Macaca mulatta	D1LYT2	100.0%	Diamond
Drosophila melanogaster	P25123	99.8%	Diamond
Bos taurus	P57695	99.8%	Diamond
Macaca fascicularis	Q4R534	99.8%	Diamond
Pongo abelii	Q5RCC5	99.8%	Diamond
Drosophila simulans	Q9BLY8	99.8%	Diamond
Gallus gallus	P19150	96.9%	Diamond
Musca domestica	Q75NA5	84.3%	Diamond
Haemonchus contortus	P91730	81.4%	Diamond
Caenorhabditis elegans	Q17328	81.4%	Diamond
Lymnaea stagnalis	P26714	58.6%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
GABRA2	protein-coding	2555
COX7B2	protein-coding	170712

Protein

Protein identifiers

Gamma-aminobutyric acid receptor subunit gamma-1 — Q8N1C3 (reviewed: Q8N1C3)

Alternative names: GABA(A) receptor subunit gamma-1

All UniProt accessions (1): Q8N1C3

UniProt curated annotations — full annotation on UniProt →

Function. Gamma subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain. GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient. Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission.

Subunit / interactions. Heteropentamer, formed by a combination of alpha (GABRA1-6), beta (GABRB1-3), gamma (GABRG1-3), delta (GABRD), epsilon (GABRE), rho (GABRR1-3), pi (GABRP) and theta (GABRQ) chains, each subunit exhibiting distinct physiological and pharmacological properties.

Subcellular location. Postsynaptic cell membrane. Cell membrane.

Post-translational modifications. May be palmitoylated.

Domain organisation. GABAARs subunits share a common topological structure: a peptide sequence made up of a long extracellular N-terminal, four transmembrane domains, intracellular or cytoplasmic domain located between the third and the fourth transmembrane domains.

Similarity. Belongs to the ligand-gated ion channel (TC 1.A.9) family. Gamma-aminobutyric acid receptor (TC 1.A.9.5) subfamily. GABRG1 sub-subfamily.

RefSeq proteins (1): NP_775807* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR005437	GABRG-1-4	Family
IPR005438	GABBAg1_rcpt	Family
IPR006028	GABAA/Glycine_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)

• chloride(in) = chloride(out) (RHEA:29823)

UniProt features (15 total): topological domain 4, transmembrane region 4, glycosylation site 3, signal peptide 1, chain 1, disulfide bond 1, sequence variant 1

Structure

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8N1C3-F1	79.06	0.61

Human Protein Atlas

Protein class: Predicted membrane proteins, FDA approved drug targets, Small molecule drugs

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): plasma membrane; vesicles

Antibody reliability (HPA): IH approved · IF supported

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 (1)

Type	Positions
Disulfide bond	188–202

Glycosylation sites (3)

Type	Positions
N-linked (glcnac…) asparagine	50, 127, 245

Function

Pathways and Gene Ontology

Reactome pathways

0 curated (TAS) of 0; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

MSigDB gene sets: 167 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GOBP_SYNAPSE_ASSEMBLY, AAGCCAT_MIR135A_MIR135B, GOBP_INORGANIC_ANION_TRANSPORT, GOBP_GAMMA_AMINOBUTYRIC_ACID_SIGNALING_PATHWAY, LHX3_01, GOBP_CELL_CELL_SIGNALING, chr4p12, GOBP_CELL_JUNCTION_ORGANIZATION, GOBP_CHLORIDE_TRANSPORT, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, TGACATY_UNKNOWN, GOBP_SYNAPTIC_SIGNALING, AACTTT_UNKNOWN, GOBP_CELL_JUNCTION_ASSEMBLY

GO Biological Process (7): gamma-aminobutyric acid signaling pathway (GO:0007214), synaptic transmission, GABAergic (GO:0051932), chloride transmembrane transport (GO:1902476), inhibitory synapse assembly (GO:1904862), monoatomic ion transport (GO:0006811), chloride transport (GO:0006821), monoatomic ion transmembrane transport (GO:0034220)

GO Molecular Function (8): GABA-A receptor activity (GO:0004890), GABA-gated chloride ion channel activity (GO:0022851), GABA receptor binding (GO:0050811), transmembrane signaling receptor activity (GO:0004888), monoatomic ion channel activity (GO:0005216), extracellular ligand-gated monoatomic ion channel activity (GO:0005230), chloride channel activity (GO:0005254), protein binding (GO:0005515)

GO Cellular Component (8): plasma membrane (GO:0005886), dendrite membrane (GO:0032590), chloride channel complex (GO:0034707), postsynaptic membrane (GO:0045211), postsynapse (GO:0098794), GABA-A receptor complex (GO:1902711), membrane (GO:0016020), signaling receptor complex (GO:0043235)

GO top-level categories

33 GO namespaces:

Category	Terms
GABA receptor activity	2
cellular anatomical structure	2
cell-cell signaling	1
chemical synaptic transmission	1
chloride transport	1
monoatomic anion transmembrane transport	1
synapse assembly	1
transport	1
monoatomic anion transport	1
inorganic anion transport	1
monoatomic ion transport	1
transmembrane transport	1
chloride channel activity	1
transmitter-gated monoatomic ion channel activity	1
ligand-gated monoatomic anion channel activity	1
signaling receptor binding	1
signaling receptor activity	1
monoatomic ion transmembrane transporter activity	1
channel activity	1
ligand-gated monoatomic ion channel activity	1
monoatomic anion channel activity	1
chloride transmembrane transporter activity	1
binding	1
membrane	1
cell periphery	1
dendrite	1
neuron projection membrane	1
monoatomic ion channel complex	1
synaptic membrane	1
postsynapse	1
synapse	1
GABA receptor complex	1
protein-containing complex	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 1 of 23 annotations. The rest are phylogenetic / computational / electronic (IEA).

1 experimentally-supported GO terms:

GO term	NS	Evidence
plasma membrane	CC	direct assay

Protein interactions and networks

STRING

showing 17 of 1,418 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GABRG1	OPRD1	P41143	505
GABRG1	GABRB1	P18505	471
GABRG1	GABRA2	P47869	451
GABRG1	OPRM1	P35372	435
GABRG1	DRD2	P14416	423
GABRG1	PGM1	P36871	420
GABRG1	GABBR2	O75899	413
GABRG1	TTC12	Q9H892	399
GABRG1	NPY2R	P49146	395
GABRG1	CHRM2	P08172	389
GABRG1	GABRA4	P48169	382
GABRG1	SCN1B	Q07699	380
GABRG1	GRIK1	P39086	371
GABRG1	HSPB6	O14558	370
GABRG1	GAPDHS	O14556	370
GABRG1	ACOT13	Q9NPJ3	370
GABRG1	GDF15	P78360	370

IntAct

Human interaction partners of GABRG1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

2 partners by confidence:

Partner	Interaction type	MIscore	Records
OPTN	physical association	0.560	3
ECE1	physical association	0.370	1

BioGRID (4 interactions; top human partners by supporting records): GABRG2 (Affinity Capture-MS; 2 records), DHRS7B (Cross-Linking-MS (XL-MS)), SHANK2 (Cross-Linking-MS (XL-MS))

Disease & clinical

Genetic variants

Variant evidence for GABRG1: 65 ClinVar records (0 pathogenic / likely pathogenic); 6 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	60
Likely benign	0
Benign	0

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 33 predictions of 695):

Position(s)	Effect	Δscore	Sites
4:46064439–46064440	donor_loss	1.0000	5
4:46064524–46064525	acceptor_loss	1.0000	3
4:46064528	acceptor_gain	1.0000
4:46083984–46083985	donor_loss	1.0000	5
4:46084054–46084055	acceptor_loss	1.0000	6
4:46084061	acceptor_gain	1.0000
4:46084066	acceptor_gain	1.0000
4:46084069	acceptor_gain	1.0000
4:46097199–46097200	donor_loss	1.0000	4
4:46097350–46097351	acceptor_loss	1.0000	6

AlphaMissense

1,608 missense substitutions predicted likely pathogenic (of 3,079 scored), across 331 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M107	9	0.946	0.998
M313	9	0.944	0.999
M197	9	0.884	0.996
D198	8	0.999	1.000
D334	8	0.998	0.999
D121	8	0.997	0.999
D112	8	0.996	0.999
F292	8	0.996	1.000
D440	8	0.996	0.998
D147	8	0.995	0.999
H159	8	0.994	0.998
F447	8	0.990	0.998
F150	8	0.989	0.999
F451	8	0.986	0.999
N152	8	0.984	0.999
F264	8	0.981	0.998
N165	8	0.979	0.999
F454	8	0.979	0.997
F195	8	0.978	1.000
F343	8	0.977	0.996

HPA cancer prognostics

RNA cancer specificity: Not detected

Disease associations

OMIM: gene MIM:137166 | disease phenotypes:

GenCC curated gene-disease

1 curated gene-disease records:

Disease	Classification	Inheritance	Records
genetic developmental and epileptic encephalopathy	Limited	Autosomal dominant	2

Mondo (1): genetic developmental and epileptic encephalopathy (MONDO:0100062)

GWAS associations

6 associations:

Study	Trait	p-value
GCST004904_112	Body mass index	3e-48
GCST004904_209	Body mass index	1e-17
GCST006462_30	Uterine fibroids	2e-11
GCST006462_31	Uterine fibroids	3e-11
GCST006462_32	Uterine fibroids	3e-11
GCST006462_50	Uterine fibroids	2e-10

EFO canonical traits (from GWAS)

1 canonical traits:

EFO ID	Trait name
EFO:0004340	body mass index

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2093872 (PROTEIN COMPLEX GROUP), CHEMBL2109243 (PROTEIN COMPLEX GROUP)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 447,242 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

15 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL3183409	APALUTAMIDE	4	4,347
CHEMBL207538	BREXANOLONE	4	1,647
CHEMBL452	CLONAZEPAM	4	33,611
CHEMBL12	DIAZEPAM	4	92,923
CHEMBL1082407	ENZALUTAMIDE	4	10,210
CHEMBL407	FLUMAZENIL	4	7,208
CHEMBL1568698	GANAXOLONE	4	1,695
CHEMBL1544	LIOTHYRONINE	4	23,991
CHEMBL454095	ABECARNIL	2	566
CHEMBL8260	BAICALEIN	2	8,718
CHEMBL268254	DELORAZEPAM	2	1,315
CHEMBL275638	FLAVONE	2	89,655
CHEMBL287631	PROGABIDE	2	3,882
CHEMBL96	GAMMA-AMINOBUTYRIC ACID	1	161,661
CHEMBL273481	MUSCIMOL	1	5,813

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: lgic — GABA_A receptors

Binding affinities (BindingDB)

380 measured of 394 human assays (394 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
6-[[3-(5-chloro-2-pyridinyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(oxan-4-yl)pyridazine-3-carboxamide	KI	0.4 nM	US-20240279218: ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM
Halcion	KI	0.68 nM
(7S)-9-(2,6-difluorophenyl)-3,7-dimethyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene	KI	2.59 nM	US-20240190889: NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 POSITIVE ALLOSTERIC MODULATORS
6,7-dichloro-5-(2-fluoro-5-hydroxy-phenyl)-1-methyl-3H-1,4-benzodiazepin-2-one (I)	KI	2.9 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(5S)-8,9-dichloro-7-(2-fluoro-5-hydroxy-phenyl)-5-methyl-5H-pyrimido[1,2-a][1,4]benzodiazepin-3-one	KI	3.3 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
4-fluoro-3-[(4S)-7,8-dichloro-1,4-dimethyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-6-yl]phenol	KI	3.35 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
6-chloro-5-(2-fluoro-5-hydroxy-phenyl)-1,7-dimethyl-3H-1,4-benzodiazepin-2-one (II)	KI	3.49 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-pyridazin-3-yl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	3.8 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
8-chloro-7-(2-fluoro-5-hydroxy-phenyl)-9-(trifluoromethyl)-5H-pyrimido[1,2-a][1,4]benzodiazepin-3-one	KI	5.17 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
6-chloro-5-(2-fluoro-5-hydroxy-phenyl)-1-methyl-7-(trifluoromethyl)-3H-1,4-benzodiazepin-2-one	KI	5.43 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
3-(7,8-dichloro-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-6-yl)-4-fluoro-phenol	KI	5.44 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-(6-methylpyridazin-3-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	5.9 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7-chloro-6-(2,6-difluorophenyl)-8-iodo-1,4-dimethyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	6.6 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
9-(2-chlorophenyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene	KI	6.6 nM	US-20240190889: NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 POSITIVE ALLOSTERIC MODULATORS
5-[(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-1-yl]-3-methyl-isoxazole	KI	8 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
[(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-3a,4-dihydro-1H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]-(1,1-dioxo-1,4-thiazinan-4-yl)methanone	KI	8.25 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
(4S)-8-bromo-7-chloro-6-(2,6-difluorophenyl)-1,4-dimethyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	8.3 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-2,4-dimethyl-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepine	KI	8.3 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
3-[7-chloro-1-methyl-8-(trifluoromethyl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-6-yl]-4-fluoro-phenol	KI	8.45 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
azetidin-1-yl-[(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]methanone	KI	8.5 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
8,9-dichloro-7-(2,6-difluorophenyl)-5H-pyrimido[1,2-a][1,4]benzodiazepin-3-one	KI	8.6 nM	US-20240287082: NEW BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
(4S)-8-bromo-7-chloro-6-(2,6-difluorophenyl)-4-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	9 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
[(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]-(3-methoxyazetidin-1-yl)methanone	KI	9.2 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-pyrimidin-4-yl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	10.2 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-(6-methylpyrimidin-4-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	10.3 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
[7-chloro-6-(2-fluoro-5-hydroxy-phenyl)-8-(trifluoromethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]-(3-methoxyazetidin-1-yl)methanone	KI	11.4 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-2,4-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-1-one	KI	11.5 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-1,4-dimethyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	12.8 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
[(4R)-8-bromo-7-chloro-6-(2,6-difluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]methanol	KI	14.3 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-(1-methylpyrazol-4-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	14.4 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(7S,13R)-13-(difluoromethyl)-9-(2,6-difluorophenyl)-3,7-dimethyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene	KI	14.4 nM	US-20240190889: NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 POSITIVE ALLOSTERIC MODULATORS
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-N-(2-hydroxyethyl)-4-methyl-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide	KI	15.2 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
(13R)-13-(difluoromethyl)-9-(2,6-difluorophenyl)-3-methyl-16-thia-2,4,5,8-tetrazatetracyclo[8.6.0.02,6.011,15]hexadeca-1(10),3,5,8,11(15)-pentaene	KI	16.8 nM	US-20240190889: NEW CYCLOPENTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 POSITIVE ALLOSTERIC MODULATORS
(5S)-9-bromo-8-chloro-7-(2,6-difluorophenyl)-5-methyl-5H-pyrimido[1,2-a][1,4]benzodiazepin-3-one	KI	17.6 nM	US-20240287082: NEW BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
(7S)-9-(2,6-difluorophenyl)-3,7-dimethyl-18-thia-2,4,5,8-tetrazatetracyclo[8.8.0.02,6.011,17]octadeca-1(10),3,5,8,11	KI	19.2 nM	US-20240294543: CYCLOHEPTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
6-[(4S)-7-chloro-2,4-dimethyl-8-(trifluoromethyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-6-yl]-5-fluoro-pyridin-2-ol	KI	19.9 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
9-(2,6-difluorophenyl)-3-methyl-18-thia-2,4,5,8-tetrazatetracyclo[8.8.0.02,6.011,17]octadeca-1(10),3,5,8,11	KI	20 nM	US-20240294543: CYCLOHEPTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
5-chloro-6-[(4S)-7-chloro-1,4-dimethyl-8-(trifluoromethyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-6-yl]pyridin-2-ol	KI	20.5 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(7S)-9-(2,6-difluorophenyl)-N-(2-hydroxy-2-methyl-propyl)-7-methyl-13,16-dioxa-18-thia-2,5,8-triazatetracyclo[8.8.0.02,6.011,17]octadeca-1(10),3,5,8,11	KI	21.7 nM	US-20240294543: CYCLOHEPTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
[(4S)-7-chloro-6-(2,6-difluorophenyl)-4-methyl-8-(trifluoromethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]-(1,1-dioxo-1,4-thiazinan-4-yl)methanone	KI	23.2 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
(4S)-7-bromo-8-chloro-6-(2,6-difluorophenyl)-4-methyl-1-(pyridazin-3-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine	KI	23.5 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(3-hydroxyazetidin-1-yl)-[(4S)-7-chloro-6-(2,6-difluorophenyl)-4-methyl-8-(trifluoromethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]methanone	KI	23.9 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-4-methyl-1-(2-methylpyrimidin-4-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	24.7 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(3-fluoroazetidin-1-yl)-[(7S)-9-(2,6-difluorophenyl)-7-methyl-13,16-dioxa-18-thia-2,3,5,8-tetrazatetracyclo[8.8.0.02,6.011,17]octadeca-1(10),3,5,8,11	KI	24.7 nM	US-20240294543: CYCLOHEPTA-THIENO-DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
6-[(4S)-7-chloro-2,4-dimethyl-8-(trifluoromethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-6-yl]-5-fluoro-pyridin-2-ol	KI	25.3 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
(5S)-8,9-dichloro-7-(2,6-difluorophenyl)-5-methyl-5H-pyrimido[1,2-a][1,4]benzodiazepin-3-one	KI	25.6 nM	US-20240287082: NEW BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM
(4S)-7,8-dichloro-6-(2,6-difluorophenyl)-1-(2,6-dimethylpyrimidin-4-yl)-4-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	27.9 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
(4S)-7-bromo-8-chloro-6-(2,6-difluorophenyl)-4-methyl-1-pyrimidin-4-yl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine	KI	28.3 nM	US-20240002393: SUBSTITUTED BENZO[f][l ,2,4JTRIAZOL0[4,3-a][l ,4JDIAZEPINES AS GABA A GAMMA! POSITIVE ALLOSTERIC MODULATORS
Estazolam	KI	28.4 nM	US-12344614: Benzodiazepine derivatives as GABA a GAMMA1 PAM
[(4S)-7-chloro-6-(2,6-difluorophenyl)-4-methyl-8-(trifluoroethyl)-4H-[1,2,4]triazolo[1,5-a][1,4]benzodiazepin-2-yl]-(3-methoxyazetidin-1-yl)methanone	KI	29 nM	US-12365687: Benzodiazepine derivatives as GABA A gamma 1 PAM

ChEMBL bioactivities

474 potent at pChembl≥5 of 511 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	IC50	0.1	nM	CHEMBL454349
9.80	IC50	0.16	nM	CHEMBL309517
9.70	IC50	0.2	nM	CHEMBL4747460
9.62	IC50	0.24	nM	CHEMBL79037
9.40	IC50	0.3981	nM	CGS-8216
9.40	IC50	0.4	nM	CHEMBL1271047
9.34	IC50	0.46	nM	CHEMBL78730
9.31	IC50	0.49	nM	CHEMBL76263
9.30	IC50	0.5	nM	CHEMBL5266498
9.30	IC50	0.5	nM	CHEMBL5290464
9.30	IC50	0.5	nM	CHEMBL5280240
9.30	IC50	0.5	nM	CHEMBL49141
9.30	IC50	0.5	nM	CHEMBL1518572
9.22	IC50	0.6026	nM	CGS-9896
9.22	IC50	0.6	nM	CHEMBL419096
9.12	IC50	0.76	nM	CHEMBL540583
9.10	IC50	0.79	nM	CHEMBL77226
9.10	IC50	0.8	nM	CHEMBL5265845
9.10	IC50	0.8	nM	CHEMBL5291368
9.10	IC50	0.8	nM	CHEMBL5271392
9.07	Ki	0.85	nM	CLONAZEPAM
9.05	Ki	0.9	nM	FLUMAZENIL
9.05	IC50	0.9	nM	CHEMBL5285377
9.00	Ki	1	nM	CHEMBL3410222
9.00	IC50	1	nM	BETA-CCM
9.00	IC50	1	nM	CHEMBL454606
9.00	IC50	1	nM	CHEMBL1337028
9.00	IC50	1	nM	CHEMBL509197
9.00	IC50	1	nM	ABECARNIL
9.00	Ki	1	nM	CHEMBL54341
9.00	Ki	1	nM	CHEMBL348367
8.96	IC50	1.1	nM	CHEMBL444586
8.77	Ki	1.7	nM	CHEMBL154342
8.74	IC50	1.8	nM	CHEMBL444050
8.70	IC50	2	nM	MUSCIMOL
8.66	IC50	2.2	nM	CHEMBL80610
8.64	IC50	2.3	nM	FIPRONIL
8.55	IC50	2.8	nM	CHEMBL75642
8.55	Ki	2.8	nM	CHEMBL372281
8.55	IC50	2.8	nM	DELORAZEPAM
8.52	Ki	3	nM	CHEMBL265547
8.52	IC50	3	nM	CHEMBL510764
8.52	IC50	3	nM	CHEMBL5266558
8.52	IC50	3	nM	CHEMBL2262044
8.52	IC50	3	nM	CHEMBL499814
8.52	IC50	3	nM	CHEMBL1161036
8.48	IC50	3.3	nM	CHEMBL75642
8.40	IC50	3.981	nM	CHEMBL301605
8.40	Ki	4	nM	CHEMBL330116
8.40	Ki	4	nM	CHEMBL3407528

PubChem BioAssay actives

409 with measured affinity, of 880 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
2-(4-methoxyphenyl)-1H-pyrazolo[4,3-c]quinolin-3-one	40988: Inhibition on Benzodiazepine receptor	ic50	0.0001	uM
ethyl 4-(methoxymethyl)-5-phenylmethoxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0002	uM
ethyl 4-methyl-5-propan-2-yloxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0004	uM
2-phenyl-3aH-pyrazolo[4,3-c]quinolin-3-one	40988: Inhibition on Benzodiazepine receptor	ic50	0.0004	uM
ethyl 4-(methoxymethyl)-6-phenylmethoxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0005	uM
ethyl 4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0005	uM
ethyl 6-methoxy-4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0005	uM
ethyl 4-(methoxymethyl)-6-propoxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0005	uM
ethyl 6-hydroxy-4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0005	uM
2-(4-chlorophenyl)-3aH-pyrazolo[4,3-c]quinolin-3-one	40988: Inhibition on Benzodiazepine receptor	ic50	0.0006	uM
5-[[3-(1,3-benzodioxol-5-yl)-6-iminopyridazin-1-yl]methyl]-1,2-thiazol-3-one;hydrobromide	72153: Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations.	ic50	0.0008	uM
propan-2-yl 16-(methoxymethyl)-3,6,11,14-tetrazatetracyclo[8.7.0.02,7.012,17]heptadeca-1(10),2,4,6,8,12,14,16-octaene-15-carboxylate	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0008	uM
propan-2-yl 4-(methoxymethyl)-6,9,14,21-tetrazapentacyclo[11.8.0.02,10.03,8.015,20]henicosa-1(21),2,4,6,8,10,12,15(20)-octaene-5-carboxylate	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0008	uM
propan-2-yl 15-(methoxymethyl)-4-propan-2-yl-5-oxa-10,13-diazatetracyclo[7.7.0.02,6.011,16]hexadeca-1(9),2(6),3,7,11,13,15-heptaene-14-carboxylate	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0008	uM
Clonazepam	239299: Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes	ki	0.0008	uM
15-(methoxymethyl)-14-(5-methyl-1,2-oxazol-3-yl)-4-propan-2-yl-5-oxa-3,10,13-triazatetracyclo[7.7.0.02,6.011,16]hexadeca-1(9),2(6),3,7,11,13,15-heptaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0009	uM
Flumazenil	239299: Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes	ki	0.0009	uM
ethyl 9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0010	uM
methyl 9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0010	uM
propyl 9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0010	uM
tert-butyl 9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0010	uM
7-chloro-5-methyl-3-(2-phenylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one	1196597: Displacement of [3H]flumazenil from rat cortex GABAA receptor BDZ binding site expressed in HEK293 cells by competition binding assay	ki	0.0010	uM
6-bromo-2-(3-nitrophenyl)chromen-4-one	72729: Binding affinity towards benzodiazepine site in GABAA receptor	ki	0.0010	uM
(2-methoxyphenyl)methyl 8-chloro-5-oxido-3,3a-dihydropyrazolo[5,1-c][1,2,4]benzotriazin-5-ium-3-carboxylate	41860: Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand	ki	0.0010	uM
propan-2-yl 4-(methoxymethyl)-6-phenylmethoxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0010	uM
(2-methoxyphenyl)methyl 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine-3-carboxylate	41860: Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand	ki	0.0017	uM
5-(aminomethyl)-1,2-oxazol-3-one	72155: Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection.	ic50	0.0020	uM
Fipronil	242615: In vitro insecticidal activity as inhibition of [3H]EBOB binding to Gamma-aminobutyric acid GABA-A receptor of housefly neuronal membranes	ic50	0.0023	uM
9-chloro-2-phenyl-6H-triazolo[1,2-a][1,2,4]benzotriazine-1,5-dione	239299: Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes	ki	0.0028	uM
7-chloro-5-(2-chlorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one	40974: In vitro displacement of [3H]-diazepam from GABA-A Benzodiazepine receptor	ic50	0.0028	uM
3-isothiocyanato-9H-pyrido[3,4-b]indole	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0030	uM
9H-pyrido[3,4-b]indole-3-carbonitrile	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0030	uM
3-(6,7-difluoro-1,3-benzoxazol-2-yl)-1,3a,4,5,6,7,8,8a-octahydrocyclohepta[d]imidazol-2-one	40986: Binding affinity against GABA-A benzodiazepine receptor	ki	0.0030	uM
(5aR,7R,9aS,11aS)-2-amino-7-hydroxy-9a,11a-dimethyl-3,3a,3b,4,5,5a,6,7,8,9,9b,11-dodecahydronaphtho[2,1-e]indol-10-one	72153: Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations.	ic50	0.0030	uM
3-propoxy-9H-pyrido[3,4-b]indole	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0030	uM
1-(9H-pyrido[3,4-b]indol-3-yl)butan-1-one	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0030	uM
8-fluoro-5-methyl-3-(2-phenylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one	1196597: Displacement of [3H]flumazenil from rat cortex GABAA receptor BDZ binding site expressed in HEK293 cells by competition binding assay	ki	0.0040	uM
methyl 6-hydroxy-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0040	uM
2-phenyl-6H-[1,2,4]triazolo[1,5-c]quinazolin-5-one	40986: Binding affinity against GABA-A benzodiazepine receptor	ki	0.0040	uM
17-chloro-9,12,20-triazapentacyclo[11.7.0.02,10.03,8.014,19]icosa-1(13),2(10),3,5,7,11,14,16,18-nonaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0040	uM
5-nitro-9,12,20-triazapentacyclo[11.7.0.02,10.03,8.014,19]icosa-1(13),2(10),3,5,7,11,14,16,18-nonaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0040	uM
5-bromo-9,12,20-triazapentacyclo[11.7.0.02,10.03,8.014,19]icosa-1(13),2(10),3,5,7,11,14,16,18-nonaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0040	uM
17-methoxy-9,12,20-triazapentacyclo[11.7.0.02,10.03,8.014,19]icosa-1(13),2(10),3,5,7,11,14,16,18-nonaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0040	uM
9,12,20-triazapentacyclo[11.7.0.02,10.03,8.014,19]icosa-1(13),2(10),3,5,7,11,14,16,18-nonaene	1932305: Inhibition of GABAA receptor (unknown origin)	ic50	0.0040	uM
methyl 6-(benzylamino)-9H-pyrido[3,4-b]indole-3-carboxylate	1932290: Displacement of [3H]flunitrazepam from GABAA (unknown origin ) receptor by radioligand binding assay	ic50	0.0040	uM
Diazepam	1934094: Inhibition of GABA-A receptor (unknown origin)	ic50	0.0042	uM
4-acetyl-13-(4-chlorophenyl)-5-thia-13,14-diazatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),3-trien-12-one	40977: Binding affinity for GABA-A Benzodiazepine receptor	ki	0.0042	uM
1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-(trifluoromethylsulfinyl)pyrazole	242615: In vitro insecticidal activity as inhibition of [3H]EBOB binding to Gamma-aminobutyric acid GABA-A receptor of housefly neuronal membranes	ic50	0.0042	uM
2-amino-N-[4-chloro-2-(2-chlorobenzoyl)phenyl]acetamide	40974: In vitro displacement of [3H]-diazepam from GABA-A Benzodiazepine receptor	ic50	0.0048	uM
3-(7-fluoro-1,3-benzoxazol-2-yl)-1,3a,4,5,6,7,8,8a-octahydrocyclohepta[d]imidazol-2-one	40986: Binding affinity against GABA-A benzodiazepine receptor	ki	0.0050	uM

CTD chemical–gene interactions

10 total (human), top 10 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
CGP 52608	affects binding, increases reaction	1
Resveratrol	affects cotreatment, decreases expression	1
Air Pollutants	affects methylation, increases abundance	1
Benzo(a)pyrene	decreases methylation	1
Copper	affects cotreatment, decreases expression	1
gamma-Aminobutyric Acid	affects binding, increases activity	1
Valproic Acid	decreases methylation	1
8-Bromo Cyclic Adenosine Monophosphate	increases expression	1
Aflatoxin B1	decreases methylation	1
Particulate Matter	affects methylation, increases abundance	1

ChEMBL screening assays

188 unique, capped per target: 169 binding, 15 functional, 3 toxicity, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3363914	Binding	Displacement of [3H]Muscimol from rat GABAA receptor at 10 uM after 90 mins by microbeta counting analysis	Griseorhodins D-F, neuroactive intermediates and end products of post-PKS tailoring modification in Griseorhodin biosynthesis. — *J Nat Prod*
CHEMBL4810229	ADMET	Inhibition of GABA A 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*
CHEMBL5335653	Toxicity	Antagonist activity at GABA-A (unknown origin)	Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer. — *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_YA48	IDG-HEK293T-GABRG1-V5-OE	Transformed cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 312 trials:

NCT	Phase	Status	Title
NCT00029224	Phase 4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	Phase 4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	Phase 4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	Phase 4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	Phase 4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	Phase 4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	Phase 4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	Phase 4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	Phase 4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	Phase 4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	Phase 4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	Phase 4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	Phase 4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	Phase 4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	Phase 4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	Phase 4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	Phase 4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	Phase 4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	Phase 4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	Phase 4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	Phase 4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	Phase 4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	Phase 4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	Phase 4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	Phase 4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	Phase 4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	Phase 4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	Phase 4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	Phase 4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	Phase 4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	Phase 4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	Phase 4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	Phase 4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	Phase 4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	Phase 4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	Phase 4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	Phase 4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	Phase 4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	Phase 4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	Phase 4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer
NCT01673984	Phase 4	TERMINATED	GP Extended Action Triptorelin
NCT01753297	Phase 4	COMPLETED	A Study of Immediate 9 Months Adjuvant Hormone Therapy With Triptorelin 11.25 mg Versus Active Surveillance After Radical Prostatectomy in High Risk Prostate Cancer Patients.
NCT01794793	Phase 4	COMPLETED	Study to Allow Access to Pasireotide for Patients Benefiting From Pasireotide Treatment in Novartis-sponsored Studies
NCT01950871	Phase 4	TERMINATED	Prostate Guided Biopsy Study Evaluating the Diagnostic Performance of Prostate HistoScanning
NCT01995513	Phase 4	COMPLETED	Safety Study of Continued Enzalutamide Treatment In Prostate Cancer Patients
NCT02102646	Phase 4	COMPLETED	MRI Substudy; Metabolic Changes Due to Iatrogenic Hypogonadism
NCT02116582	Phase 4	COMPLETED	A Study to Evaluate Enzalutamide After Abiraterone in Metastatic Castration-Resistant Prostate Cancer
NCT02149628	Phase 4	COMPLETED	The Effect of Propofol Based Total Intravenous Anesthesia on Oxidative Stress and Nitric Oxide
NCT02405858	Phase 4	COMPLETED	A Study of Abiraterone Acetate in Metastatic Castration-Resistant Prostate Cancer Participants Who Responded Poorly to the First-line Combined Androgen Blockade Therapy
NCT02441517	Phase 4	TERMINATED	A Study of Enzalutamide Re-treatment in Metastatic Castration-resistant Prostate Cancer After Docetaxel and/or Cabazitaxel Treatment
NCT02441894	Phase 4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT02475057	Phase 4	COMPLETED	Endothelial Function in Prostate Cancer Patients on Degarelix vs. Luteinizing Hormone-Releasing Hormone Agonists
NCT02511665	Phase 4	UNKNOWN	Metformin And Longevity
NCT02651948	Phase 4	COMPLETED	Transperineal, MRI-guided, Prostate Biopsy
NCT02721433	Phase 4	COMPLETED	4-weekly Versus 12-weekly Administration of Bone-targeted Agents in Patients With Bone Metastases
NCT02726009	Phase 4	COMPLETED	A Trial to Evaluate Safety of Firmagon® (Degarelix) in Indian Patients Diagnosed With Advanced Hormone-dependent Prostate Cancer
NCT02749825	Phase 4	TERMINATED	Comparison of Trelstar Versus Lupron or Zoladex in Advanced Prostate Cancer
NCT02757365	Phase 4	UNKNOWN	Efficiency Study of Aspirin to Prevent the Occurrence of Prostate Cancer
NCT02773251	Phase 4	COMPLETED	The Effect of Guardix-solution for the Prevention of Postoperative Intestinal Adhesion and Intestinal Obstruction After Laparoscopic Pelvic Cavity Surgery
NCT02812186	Phase 4	COMPLETED	Deep Versus Moderate Neuromuscular Blockade During Laparoscopic Surgery

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for GABRG1 across ~30M SureChEMBL compounds — explore on Sugi Predict.