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Assay Detail

CHEMBL2065550

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 cells
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

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.
Luo G, Chen L, Conway CM, Denton R, Keavy D, Gulianello M, Huang Y, Kostich W, Lentz KA, Mercer SE, Schartman R, Signor L, Browning M, Macor JE, Dubowchik GM.
ACS Med Chem Lett (2012) 3 : 337 -341
PubMed 24900474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.33 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207197 OLCEGEPANT 2.0 1 11.00
CHEMBL2023191 1 10.15
CHEMBL2063115 1 10.15
CHEMBL2063116 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207197 OLCEGEPANT Ki = 0.01 nM 11.00
CHEMBL2023191 Ki = 0.071 nM 10.15
CHEMBL2063115 Ki = 0.07 nM 10.15
CHEMBL2063116 Ki = 940.0 nM 6.03