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Assay Detail

CHEMBL998691

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

Functional
Ex vivo effect on basal artery tension in human coronary artery assessed as contractility
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Coronary artery
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.
Degnan AP, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Denton R, Han X, Macci R, Mathias NR, Moench P, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Macor JE, Dubowchik GM.
J Med Chem (2008) 51 : 4858 -4861
PubMed 18665579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.51 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL450668 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL450668 EC50 = 311.0 nM 6.51