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Assay Detail

CHEMBL1070098

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

Binding
Displacement of [3H]epibatidine from alpha3beta4 nAChR expressed in IMR32 cells
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IMR-32
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594)
Type PROTEIN COMPLEX
Organism Homo sapiens

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 5.27 5.27
IC50 1 7.81 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365956 1 7.81
CHEMBL604798 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365956 IC50 = 15.6 nM 7.81
CHEMBL604798 Ki = 5370.0 nM 5.27