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Assay Detail

CHEMBL3424812

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Binding
Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by fluorescent calcium assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type GH4-C1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
Beinat C, Reekie T, Banister SD, O'Brien-Brown J, Xie T, Olson TT, Xiao Y, Harvey A, O'Connor S, Coles C, Grishin A, Kolesik P, Tsanaktsidis J, Kassiou M.
Eur J Med Chem (2015) 95 : 277 -301
PubMed 25827398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.49 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082655 1 7.60
CHEMBL3422596 1 6.90
CHEMBL3422581 1 6.84
CHEMBL3422597 1 6.60
CHEMBL3422580 1 6.28
CHEMBL1084615 1 6.16
CHEMBL3422582 1 6.00
CHEMBL576234 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082655 EC50 = 25.0 nM 7.60
CHEMBL3422596 EC50 = 126.0 nM 6.90
CHEMBL3422581 EC50 = 145.0 nM 6.84
CHEMBL3422597 EC50 = 253.0 nM 6.60
CHEMBL3422580 EC50 = 522.0 nM 6.28
CHEMBL1084615 EC50 = 687.0 nM 6.16
CHEMBL3422582 EC50 = 997.0 nM 6.00
CHEMBL576234 EC50 = 2840.0 nM 5.55