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Assay Detail

CHEMBL2400790

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-CGRP from CGRP receptor in human SK-N-MC cell membranes after 2 hrs by scintillation counting analysis
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calcitonin gene-related peptide type 1 receptor (CHEMBL3798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.
Chaturvedula PV, Mercer SE, Pin SS, Thalody G, Xu C, Conway CM, Keavy D, Signor L, Cantor GH, Mathias N, Moench P, Denton R, Macci R, Schartman R, Whiterock V, Davis C, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2013) 23 : 3157 -3161
PubMed 23632269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 10.64 10.64
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2397415 ZAVEGEPANT 4.0 2 10.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2397415 ZAVEGEPANT Ki = 0.023 nM 10.64
CHEMBL2397415 ZAVEGEPANT Inhibition - % -