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Assay Detail

CHEMBL2157808

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Functional
Agonist activity at alpha7 nAChR
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of α7 nicotinic acetylcholine receptor modulators.
Mazurov AA, Speake JD, Yohannes D.
J Med Chem (2011) 54 : 7943 -7961
PubMed 21919481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.75 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378471 1 7.37
CHEMBL378349 1 7.32
CHEMBL1258005 1 7.30
CHEMBL379302 1 7.07
CHEMBL212669 1 7.00
CHEMBL1086089 1 6.92
CHEMBL1084363 1 6.89
CHEMBL597241 1 6.80
CHEMBL603052 1 6.80
CHEMBL2151569 1 6.50
CHEMBL565963 1 6.46
CHEMBL56564 TROPISETRON 3.0 1 5.89
CHEMBL2151443 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378471 EC50 = 43.0 nM 7.37
CHEMBL378349 EC50 = 48.0 nM 7.32
CHEMBL1258005 EC50 = 50.0 nM 7.30
CHEMBL379302 EC50 = 86.0 nM 7.07
CHEMBL212669 EC50 = 100.0 nM 7.00
CHEMBL1086089 EC50 = 120.0 nM 6.92
CHEMBL1084363 EC50 = 130.0 nM 6.89
CHEMBL597241 EC50 = 160.0 nM 6.80
CHEMBL603052 EC50 = 160.0 nM 6.80
CHEMBL2151569 EC50 = 320.0 nM 6.50
CHEMBL565963 EC50 = 350.0 nM 6.46
CHEMBL56564 TROPISETRON EC50 = 1300.0 nM 5.89
CHEMBL2151443 EC50 = 4260.0 nM 5.37