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Assay Detail

CHEMBL2344725

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Functional
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CCRP-induced cAMP production
17
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Degnan AP, Jiang XJ, Macci R, Mathias NR, Moench P, Pin SS, Schartman R, Signor LJ, Thalody G, Tora G, Whiterock V, Xu C, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2013) 23 : 1870 -1873
PubMed 23402880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 16 - -
EC50 1 10.77 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL454791 2 10.77
CHEMBL2336411 1 -
CHEMBL2336412 1 -
CHEMBL2336413 1 -
CHEMBL2336414 1 -
CHEMBL2336415 1 -
CHEMBL2336416 1 -
CHEMBL2336417 1 -
CHEMBL2336418 1 -
CHEMBL2336419 1 -
CHEMBL2336420 1 -
CHEMBL2336421 1 -
CHEMBL2336422 1 -
CHEMBL2336423 1 -
CHEMBL2336424 1 -
CHEMBL454751 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL454791 EC50 = 0.017 nM 10.77
CHEMBL2336420 Inhibition - % -
CHEMBL2336411 Inhibition - % -
CHEMBL2336412 Inhibition - % -
CHEMBL2336413 Inhibition - % -
CHEMBL2336414 Inhibition - % -
CHEMBL2336415 Inhibition - % -
CHEMBL2336416 Inhibition - % -
CHEMBL2336417 Inhibition - % -
CHEMBL2336419 Inhibition - % -
CHEMBL2336421 Inhibition - % -
CHEMBL2336422 Inhibition - % -
CHEMBL2336423 Inhibition - % -
CHEMBL454791 Inhibition - % -
CHEMBL2336424 Inhibition - % -
CHEMBL454751 Inhibition - % -
CHEMBL2336418 Inhibition - % -