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Talnetant

Talnetant : Competitive of TACR3

Structure

Information

  • TACR3
  • Competitive
  • up to 100 nM

In Vitro Validations

Uniprot ID: P29371
Target Class: GPCR
Target SubClass: NK-3 Receptor
Potency: Ki
Potency Value: 1 nM
Potency Assay: Inhibition of [3H]-senktide binding on hNK-3r-CHO cell membranes
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Neuromedin-K receptor, TAC3R, NK3R, TACR3, NK3R_HU ...

PMID Reference: 9190866

Uniprot ID: P29371
Target Class: GPCR
Target SubClass: NK-3 Receptor
Potency: Kd
Potency Value: 1.6 ± 0.53 nM
Potency Assay: Senktide-induced contraction in isolated rabbit iris sphincter muscle
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Neuromedin-K receptor, TAC3R, NK3R, TACR3, NK3R_HU ...

PMID Reference: 9190866

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Withing target family: Selectivity relative to other tachykinin receptors was assessed by competitive binding experiments using membranes prepared from CHO cells stably expressing the human NK-2 (CHO hNK-2) and human NK-1 (CHO hNK-1) cells and [125I]NKA and [3H]substance P, respectively. Outside target family: The selectivity of SB223412 was further assessed comprehensively by testing it in >60 receptor binding, enzyme and ion channel assays. SB 223412, at concentrations up to 1 or 10 μM, was without effect in this battery of assays, except for the peripheral benzodiazepine and N-formyl-Met Leu Phe (fMLP) receptor binding assays, in which it had IC50 values of ∼1 μM (n = 2) and −3.1 ± 0.1 μM (n = 3), respectively.
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