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Assay Detail

CHEMBL5511306

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

Binding
Partial agonist activity at human alpha9 nAChR expressed as xenopus laevis oocytes assessed as increase in receptor desensitization measured after 120 secs by two-electrode voltage-clamp electrophysiology method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor subunit alpha-9 (CHEMBL2184)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.
Andleeb H, Papke RL, Stokes C, Richter K, Herz SM, Chiang K, Kanumuri SRR, Sharma A, Damaj MI, Grau V, Horenstein NA, Thakur GA.
J Med Chem (2024) 67 : 8642 -8666
PubMed 38748608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.15 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561901 1 5.95
CHEMBL5557858 1 5.16
CHEMBL5542521 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561901 EC50 = 1120.0 nM 5.95
CHEMBL5557858 EC50 = 7000.0 nM 5.16
CHEMBL5542521 EC50 = 45000.0 nM 4.35