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TargetCholinergic receptors

Neuronal acetylcholine receptor; alpha4/beta2

Muscarinic and nicotinic acetylcholine receptors.

Measurements
9
Compounds
4
Binding constants
6
Median pX
6.57

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 Neuronal acetylcholine receptor; alpha4/beta2. 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.

  1. 01Arecoline6.57

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 6

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

TargetClassTypeValue (nM)pXOrganismAssay
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi2706.57Rattus norvegicusCHEMBL756007
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi2706.57Rattus norvegicusCHEMBL756005
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi— no normalized value— value does not convert to pXRattus norvegicusCHEMBL896280
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2396008
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2396009
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsKi— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3271085

Functional readouts 1

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

TargetClassTypeValue (nM)pXOrganismAssay
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsIC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3271084

Other measurements 2

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.

TargetClassTypeValue (nM)pXOrganismAssay
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsInhibition— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3271084
Neuronal acetylcholine receptor; alpha4/beta2Cholinergic receptorsActivity— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3271087