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Assay Detail

CHEMBL2026486

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

Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
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

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.
Luo G, Chen L, Civiello R, Pin SS, Xu C, Kostich W, Kelley M, Conway CM, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2012) 22 : 2917 -2921
PubMed 22429470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.11 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023191 1 9.74
CHEMBL2023188 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023191 Ki = 0.18 nM 9.74
CHEMBL2023188 Ki = 3.3 nM 8.48