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Assay Detail

CHEMBL5511331

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

Functional
Inhibition of ATP-mediated IL-1beta release in LPS primed BzATP induced monocytic human THP-1 cells primed with LPS for 5 hrs followed by BzATP and compound addition for 40 mins by ELISA
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 3 5.40 6.30
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5558610 2 6.30
CHEMBL5555218 2 5.05
CHEMBL5556786 2 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5558610 IC50 = 500.0 nM 6.30
CHEMBL5555218 IC50 = 9000.0 nM 5.05
CHEMBL5556786 IC50 = 14000.0 nM 4.85
CHEMBL5556786 Inhibition - % -
CHEMBL5555218 Inhibition - % -
CHEMBL5558610 Inhibition - % -