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Assay Detail

CHEMBL869736

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

Functional
Activity at alpha7-5HT3 chimera expressed in SHEP1 cells by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SHEP1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 16 6.86 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378471 1 7.33
CHEMBL378349 1 7.32
CHEMBL208565 1 7.26
CHEMBL214268 PHA-543613 1.0 1 7.19
CHEMBL378496 1 7.11
CHEMBL268939 1 7.09
CHEMBL379302 1 7.07
CHEMBL210865 1 7.00
CHEMBL212669 1 7.00
CHEMBL177611 PNU-282987 1 6.89
CHEMBL214195 1 6.43
CHEMBL377036 1 6.26
CHEMBL211572 1 6.22
CHEMBL377032 1 5.93
CHEMBL214243 1 -
CHEMBL375776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378471 EC50 = 47.0 nM 7.33
CHEMBL378349 EC50 = 48.0 nM 7.32
CHEMBL208565 EC50 = 55.0 nM 7.26
CHEMBL214268 PHA-543613 EC50 = 65.0 nM 7.19
CHEMBL378496 EC50 = 77.0 nM 7.11
CHEMBL268939 EC50 = 81.0 nM 7.09
CHEMBL379302 EC50 = 86.0 nM 7.07
CHEMBL210865 EC50 = 100.0 nM 7.00
CHEMBL212669 EC50 = 100.0 nM 7.00
CHEMBL177611 PNU-282987 EC50 = 128.0 nM 6.89
CHEMBL214195 EC50 = 374.0 nM 6.43
CHEMBL377036 EC50 = 550.0 nM 6.26
CHEMBL211572 EC50 = 600.0 nM 6.22
CHEMBL377032 EC50 = 1173.0 nM 5.93
CHEMBL214243 EC50 > 10000.0 nM -
CHEMBL375776 EC50 > 10000.0 nM -