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Assay Detail

CHEMBL1212431

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

Binding
Positive allosteric modulator activity at human alpha7 nAChR expressed in rat GH4C1 assessed as calcium mobilization by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.
Capelli AM, Castelletti L, Salvagno C, Oliosi B, Di Lenarda E, Virginio C, Lightfoot A, Kew JN, Teague S.
Bioorg Med Chem Lett (2010) 20 : 4561 -4565
PubMed 20591663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.62 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1210516 1 8.70
CHEMBL1210515 1 8.70
CHEMBL1210517 1 8.50
CHEMBL1210576 1 8.20
CHEMBL1210577 1 8.10
CHEMBL1210579 1 8.00
CHEMBL1210578 1 8.00
CHEMBL1210518 1 8.00
CHEMBL1210643 1 7.60
CHEMBL1210642 1 7.60
CHEMBL1210641 1 7.60
CHEMBL1210640 1 7.50
CHEMBL257591 1 6.80
CHEMBL1210703 1 6.80
CHEMBL1210702 1 5.90
CHEMBL1210458 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1210516 EC50 = 1.995 nM 8.70
CHEMBL1210515 EC50 = 1.995 nM 8.70
CHEMBL1210517 EC50 = 3.162 nM 8.50
CHEMBL1210576 EC50 = 6.31 nM 8.20
CHEMBL1210577 EC50 = 7.943 nM 8.10
CHEMBL1210579 EC50 = 10.0 nM 8.00
CHEMBL1210578 EC50 = 10.0 nM 8.00
CHEMBL1210518 EC50 = 10.0 nM 8.00
CHEMBL1210643 EC50 = 25.12 nM 7.60
CHEMBL1210642 EC50 = 25.12 nM 7.60
CHEMBL1210641 EC50 = 25.12 nM 7.60
CHEMBL1210640 EC50 = 31.62 nM 7.50
CHEMBL257591 EC50 = 158.49 nM 6.80
CHEMBL1210703 EC50 = 158.49 nM 6.80
CHEMBL1210702 EC50 = 1258.93 nM 5.90
CHEMBL1210458 EC50 = 1258.93 nM 5.90