Assay Detail

CHEMBL2400792

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Functional

Reversal of CGRP-induced dilation of human intracranial arterial rings

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

Chaturvedula PV, Mercer SE, Pin SS, Thalody G, Xu C, Conway CM, Keavy D, Signor L, Cantor GH, Mathias N, Moench P, Denton R, Macci R, Schartman R, Whiterock V, Davis C, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2013) 23 : 3157 -3161
PubMed 23632269 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	9.06	9.06

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2397415	ZAVEGEPANT	4.0	1	9.06

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2397415	ZAVEGEPANT	EC50	=	0.88	nM	9.06