TargetGABA receptors

GABAA

GABA-A and GABA-B receptors.

Measurements: 51
Compounds: 9
Binding constants: 23
Median pX: 8.21

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

No single gene answers to GABAA. Names like this one are families or unsubtyped preparations — a measurement made against whatever receptors a tissue carried, before or without resolving which subtype bound the compound. A family has no one accession, and picking a member to stand for it would invent a precision the assay never had: asked for “Muscarinic acetylcholine receptor” UniProt returns CHRM1, and that answer is wrong.

Resolver said no gene lists this target name as a synonym — recorded by tools/fetch_expression.py, not written here.

III · Ranking

Compounds by strongest binding constant

One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 23

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

Target	Class	Type	Value (nM)	pX	Organism	Assay
GABAA	GABA receptors	Ki	1.30	8.89	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	2.88	8.54	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	4.00	8.40	Rattus norvegicus	CHEMBL680229
GABAA	GABA receptors	Ki	4.30	8.37	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	4.57	8.34	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	5.00	8.30	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	5.37	8.27	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	5.75	8.24	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	6.00	8.22	Homo sapiens	CHEMBL3370250
GABAA	GABA receptors	Ki	6.10	8.21	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	6.76	8.17	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	6.80	8.17	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	8.31	8.08	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	8.40	8.08	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	8.91	8.05	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	9.10	8.04	HUMAN	PMID 9396785
GABAA	GABA receptors	Ki	11.00	7.96	Homo sapiens	CHEMBL681334
GABAA	GABA receptors	Ki	1,620	5.79	Rattus norvegicus	CHEMBL652562
GABAA	GABA receptors	Ki	12,400	4.91	Rattus norvegicus	CHEMBL652562
GABAA	GABA receptors	Ki	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL652562
GABAA	GABA receptors	Ki	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL652455
GABAA	GABA receptors	Ki	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL652455
GABAA	GABA receptors	Ki	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL652562

Show all 23 rowsShow first 20

Functional readouts 24

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

Target	Class	Type	Value (nM)	pX	Organism	Assay
GABAA	GABA receptors	IC50	3.00	8.52	Rattus norvegicus	CHEMBL681302
GABAA	GABA receptors	IC50	3.20	8.49	Rattus norvegicus	CHEMBL681130
GABAA	GABA receptors	IC50	5.00	8.30	Rattus norvegicus	CHEMBL681138
GABAA	GABA receptors	IC50	6.00	8.22	Rattus norvegicus	CHEMBL681137
GABAA	GABA receptors	IC50	6.00	8.22	Rattus norvegicus	CHEMBL681241
GABAA	GABA receptors	IC50	10.00	8.00	Rattus norvegicus	CHEMBL681240
GABAA	GABA receptors	IC50	16.00	7.80	Homo sapiens	CHEMBL881988
GABAA	GABA receptors	IC50	1,600	5.80	Homo sapiens	CHEMBL5235566
GABAA	GABA receptors	IC50	1,620	5.79	Rattus norvegicus	CHEMBL650289
GABAA	GABA receptors	IC50	1,620	5.79	Rattus norvegicus	CHEMBL650178
GABAA	GABA receptors	IC50	1,622	5.79	Rattus norvegicus	CHEMBL651677
GABAA	GABA receptors	IC50	1,622	5.79	Rattus norvegicus	CHEMBL858255
GABAA	GABA receptors	IC50	1,622	5.79	Homo sapiens	CHEMBL650075
GABAA	GABA receptors	IC50	2,500	5.60	Homo sapiens	CHEMBL5235566
GABAA	GABA receptors	IC50	12,303	4.91	Homo sapiens	CHEMBL650075
GABAA	GABA receptors	IC50	12,388	4.91	Rattus norvegicus	CHEMBL651677
GABAA	GABA receptors	IC50	12,388	4.91	Rattus norvegicus	CHEMBL858255
GABAA	GABA receptors	IC50	12,400	4.91	Rattus norvegicus	CHEMBL650289
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL679565
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5235566
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5235566
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL681951
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL681949
GABAA	GABA receptors	IC50	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL5235566

Show all 24 rowsShow first 20

Other measurements 4

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

Target	Class	Type	Value (nM)	pX	Organism	Assay
GABAA	GABA receptors	Inhibition	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL650182
GABAA	GABA receptors	Inhibition	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL681304
GABAA	GABA receptors	Displacement	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL682053
GABAA	GABA receptors	Relative affinity	— no normalized value	— value does not convert to pX	Rattus norvegicus	CHEMBL681817

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