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Assay Detail

CHEMBL696021

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

Functional
In vitro inhibition of PLS- induced TNF-alpha production in human whole blood (HWB)
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Friesen RW, Ducharme Y, Ball RG, Blouin M, Boulet L, Côté B, Frenette R, Girard M, Guay D, Huang Z, Jones TR, Laliberté F, Lynch JJ, Mancini J, Martins E, Masson P, Muise E, Pon DJ, Siegl PK, Styhler A, Tsou NN, Turner MJ, Young RN, Girard Y.
J Med Chem (2003) 46 : 2413 -2426
PubMed 12773045 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.27 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112296 1 7.70
CHEMBL2112295 1 7.70
CHEMBL276559 2 7.22
CHEMBL81491 1 7.22
CHEMBL310303 1 7.05
CHEMBL199015 1 7.05
CHEMBL78806 1 6.92
CHEMBL78439 2 6.70
CHEMBL2112294 1 6.58
CHEMBL417776 2 6.19
CHEMBL61191 1 5.93
CHEMBL383762 1 5.58
CHEMBL32442 CDP840 1 4.79
CHEMBL82663 SIBENADET 2.0 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112295 IC50 = 20.0 nM 7.70
CHEMBL2112296 IC50 = 20.0 nM 7.70
CHEMBL276559 IC50 = 60.0 nM 7.22
CHEMBL81491 IC50 = 60.0 nM 7.22
CHEMBL310303 IC50 = 90.0 nM 7.05
CHEMBL199015 IC50 = 90.0 nM 7.05
CHEMBL78806 IC50 = 120.0 nM 6.92
CHEMBL78439 IC50 = 200.0 nM 6.70
CHEMBL2112294 IC50 = 260.0 nM 6.58
CHEMBL417776 IC50 = 640.0 nM 6.19
CHEMBL61191 IC50 = 1180.0 nM 5.93
CHEMBL383762 IC50 = 2640.0 nM 5.58
CHEMBL276559 IC50 = 3520.0 nM 5.45
CHEMBL417776 IC50 = 9010.0 nM 5.04
CHEMBL32442 CDP840 IC50 = 16200.0 nM 4.79
CHEMBL78439 IC50 = 17900.0 nM 4.75
CHEMBL82663 SIBENADET IC50 = 18000.0 nM 4.75