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Assay Detail

CHEMBL3292879

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

Binding
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
4
Total Activities
4
Compounds Tested
1
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

Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Dasgupta B, Kozlowski E, Schroeder DR, Torrente JR, Xu C, Pin S, Conway CM, Dubowchik GM, Macor JE, Vrudhula VM.
Bioorg Med Chem Lett (2014) 24 : 2744 -2748
PubMed 24794104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.61 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207197 OLCEGEPANT 2.0 1 10.59
CHEMBL3288288 1 9.82
CHEMBL3288289 1 7.02
CHEMBL3288290 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207197 OLCEGEPANT EC50 = 0.026 nM 10.59
CHEMBL3288288 EC50 = 0.15 nM 9.82
CHEMBL3288289 EC50 = 96.0 nM 7.02
CHEMBL3288290 EC50 = 100.0 nM 7.00