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Assay Detail

CHEMBL1037633

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Functional
Agonist activity at guinea pig NK3 receptor expressed in cells assessed as accumulation of [3H]inositol phosphate
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neuromedin-K receptor (CHEMBL3799)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
Malherbe P, Kratzeisen C, Marcuz A, Zenner MT, Nettekoven MH, Ratni H, Wettstein JG, Bissantz C.
J Med Chem (2009) 52 : 7103 -7112
PubMed 19817444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 9.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL583102 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL583102 EC50 = 0.6 nM 9.22