Assay Detail

CHEMBL4833536

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Functional

Anti-hypertrophic cardiomyopathy in po dosed Sprague-Dawley rat assessed as reduction in fractional shortening measured upto 24 hrs by echocardiography

ChEMBL ↗

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Target

Rattus norvegicus (CHEMBL376) ↗

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Rattus norvegicus (CHEMBL376) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Rattus norvegicus

CHEMBL376

Anchored from Assay target.

Protein identity Rattus norvegicus

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	Rattus norvegicus
Confidence	1 — Organism
Curated By	Autocuration

Target

Rattus norvegicus (CHEMBL376) ↗

Type	ORGANISM
Organism	Rattus norvegicus

Publication

Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.

Chuang C, Collibee S, Ashcraft L, Wang W, Vander Wal M, Wang X, Hwee DT, Wu Y, Wang J, Chin ER, Cremin P, Zamora J, Hartman J, Schaletzky J, Wehri E, Robertson LA, Malik FI, Morgan BP.
J Med Chem (2021) 64 : 14142 -14152
PubMed 34606259 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.16	6.22
IC15	2	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4297517	MAVACAMTEN	4.0	2	6.22
CHEMBL4847050	AFICAMTEN	3.0	2	6.10

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4297517	MAVACAMTEN	IC50	=	600.0	nM	6.22
CHEMBL4847050	AFICAMTEN	IC50	=	800.0	nM	6.10
CHEMBL4847050	AFICAMTEN	IC15	=	7.9	uM	-
CHEMBL4297517	MAVACAMTEN	IC15	=	1.7	uM	-