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Assay Detail

CHEMBL3124573

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

Binding
Binding affinity to adenosine A2A receptor (unknown origin)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 1 5.21 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3122212 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3122212 Ki = 6100.0 nM 5.21