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Assay Detail

CHEMBL2024804

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

Functional
Agonist activity at human alpha7 nAChR expressed in GH4C1 cells by FLIPR assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type GH4-C1
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 a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, Wilson DM.
Bioorg Med Chem Lett (2012) 22 : 3560 -3563
PubMed 22503248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.46 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022495 1 7.30
CHEMBL2022496 1 7.20
CHEMBL2023927 1 7.00
CHEMBL2022939 1 7.00
CHEMBL2023930 1 6.90
CHEMBL2023928 1 6.90
CHEMBL2023919 1 6.80
CHEMBL2022499 1 6.80
CHEMBL2022938 1 6.70
CHEMBL2022935 1 6.70
CHEMBL2023929 1 6.70
CHEMBL2023924 1 6.70
CHEMBL2023917 1 6.60
CHEMBL2021948 1 6.60
CHEMBL2022497 1 6.50
CHEMBL2023916 1 6.50
CHEMBL2022940 1 6.40
CHEMBL2023925 1 6.40
CHEMBL2023920 1 6.30
CHEMBL2023926 1 6.30
CHEMBL2022941 1 6.20
CHEMBL2023918 1 6.00
CHEMBL2023921 1 5.90
CHEMBL2023923 1 5.70
CHEMBL2023922 1 5.50
CHEMBL2022936 1 5.40
CHEMBL2022937 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022495 EC50 = 50.12 nM 7.30
CHEMBL2022496 EC50 = 63.1 nM 7.20
CHEMBL2023927 EC50 = 100.0 nM 7.00
CHEMBL2022939 EC50 = 100.0 nM 7.00
CHEMBL2023930 EC50 = 125.89 nM 6.90
CHEMBL2023928 EC50 = 125.89 nM 6.90
CHEMBL2023919 EC50 = 158.49 nM 6.80
CHEMBL2022499 EC50 = 158.49 nM 6.80
CHEMBL2022938 EC50 = 199.53 nM 6.70
CHEMBL2022935 EC50 = 199.53 nM 6.70
CHEMBL2023929 EC50 = 199.53 nM 6.70
CHEMBL2023924 EC50 = 199.53 nM 6.70
CHEMBL2023917 EC50 = 251.19 nM 6.60
CHEMBL2021948 EC50 = 251.19 nM 6.60
CHEMBL2022497 EC50 = 316.23 nM 6.50
CHEMBL2023916 EC50 = 316.23 nM 6.50
CHEMBL2022940 EC50 = 398.11 nM 6.40
CHEMBL2023925 EC50 = 398.11 nM 6.40
CHEMBL2023920 EC50 = 501.19 nM 6.30
CHEMBL2023926 EC50 = 501.19 nM 6.30
CHEMBL2022941 EC50 = 630.96 nM 6.20
CHEMBL2023918 EC50 = 1000.0 nM 6.00
CHEMBL2023921 EC50 = 1258.93 nM 5.90
CHEMBL2023923 EC50 = 1995.26 nM 5.70
CHEMBL2023922 EC50 = 3162.28 nM 5.50
CHEMBL2022936 EC50 = 3981.07 nM 5.40
CHEMBL2022937 EC50 = 5011.87 nM 5.30