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Assay Detail

CHEMBL870923

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

Functional
Activity at 5HT3 receptor expressed in SHEP1 cells by FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SHEP1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
Wishka DG, Walker DP, Yates KM, Reitz SC, Jia S, Myers JK, Olson KL, Jacobsen EJ, Wolfe ML, Groppi VE, Hanchar AJ, Thornburgh BA, Cortes-Burgos LA, Wong EH, Staton BA, Raub TJ, Higdon NR, Wall TM, Hurst RS, Walters RR, Hoffmann WE, Hajos M, Franklin S, Carey G, Gold LH, Cook KK, Sands SB, Zhao SX, Soglia JR, Kalgutkar AS, Arneric SP, Rogers BN.
J Med Chem (2006) 49 : 4425 -4436
PubMed 16821801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.11 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378349 1 6.73
CHEMBL378471 1 6.24
CHEMBL214268 PHA-543613 1.0 1 6.20
CHEMBL379302 1 6.02
CHEMBL177611 PNU-282987 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378349 Ki = 188.0 nM 6.73
CHEMBL378471 Ki = 580.0 nM 6.24
CHEMBL214268 PHA-543613 Ki = 628.0 nM 6.20
CHEMBL379302 Ki = 962.0 nM 6.02
CHEMBL177611 PNU-282987 Ki = 4540.0 nM 5.34