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Assay Detail

CHEMBL2187899

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

Functional
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL6 production
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK.
Bioorg Med Chem Lett (2012) 22 : 2968 -2972
PubMed 22437115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.46 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2017288 1 7.00
CHEMBL2017285 1 7.00
CHEMBL2017281 1 7.00
CHEMBL2017291 1 6.70
CHEMBL2017286 1 6.50
CHEMBL2017273 1 6.30
CHEMBL2181820 1 6.10
CHEMBL2017277 1 6.00
CHEMBL2017269 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2017288 IC50 = 100.0 nM 7.00
CHEMBL2017285 IC50 = 100.0 nM 7.00
CHEMBL2017281 IC50 = 100.0 nM 7.00
CHEMBL2017291 IC50 = 199.53 nM 6.70
CHEMBL2017286 IC50 = 316.23 nM 6.50
CHEMBL2017273 IC50 = 501.19 nM 6.30
CHEMBL2181820 IC50 = 794.33 nM 6.10
CHEMBL2017277 IC50 = 1000.0 nM 6.00
CHEMBL2017269 IC50 = 3162.28 nM 5.50