Assay Detail

CHEMBL3124509

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

Functional

In vivo mGluR5 receptor occupancy in sc dosed Sprague-Dawley rat brain assessed as inhibition of [3H]MPEPy binding after 60 mins by liquid scintillation counting analysis

ChEMBL ↗

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Target

Rattus norvegicus (CHEMBL376) ↗

Open DB target context

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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 and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.

Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL.
J Med Chem (2014) 57 : 861 -877
PubMed 24392688 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.98	8.98

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3122212	—	—	1	8.98

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3122212	—	IC50	=	1.04	nM	8.98