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Assay Detail

CHEMBL1069500

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

Binding
Displacement of [3H]nicotine from alpha4beta2 nAChR in rat brain homogenate
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
O'Donnell CJ, Rogers BN, Bronk BS, Bryce DK, Coe JW, Cook KK, Duplantier AJ, Evrard E, Hajós M, Hoffmann WE, Hurst RS, Maklad N, Mather RJ, McLean S, Nedza FM, O'Neill BT, Peng L, Qian W, Rottas MM, Sands SB, Schmidt AW, Shrikhande AV, Spracklin DK, Wong DF, Zhang A, Zhang L.
J Med Chem (2010) 53 : 1222 -1237
PubMed 20043678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.87 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL604798 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL604798 Ki = 1350.0 nM 5.87