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Assay Detail

CHEMBL3783190

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

Functional
Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced of CXCL8 production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control
50
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.
Onions ST, Ito K, Charron CE, Brown RJ, Colucci M, Frickel F, Hardy G, Joly K, King-Underwood J, Kizawa Y, Knowles I, Murray PJ, Novak A, Rani A, Rapeport G, Smith A, Strong P, Taddei DM, Williams JG.
J Med Chem (2016) 59 : 1727 -1746
PubMed 26800309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 30 - -
IC50 20 7.69 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781245 2 8.70
CHEMBL3781473 2 8.52
CHEMBL3780667 2 8.30
CHEMBL3695568 JNJ-49095397 2.0 2 8.15
CHEMBL3780386 2 8.10
CHEMBL3781982 2 8.05
CHEMBL3780519 2 8.05
CHEMBL3781687 2 8.05
CHEMBL3781532 2 8.00
CHEMBL3781102 2 7.92
CHEMBL3781413 2 7.85
CHEMBL3780832 2 7.82
CHEMBL3780410 2 7.52
CHEMBL3781587 2 7.50
CHEMBL3780154 2 7.43
CHEMBL3781244 2 7.43
CHEMBL3780714 2 7.39
CHEMBL3782009 2 7.06
CHEMBL3781430 2 6.09
CHEMBL3781999 2 5.80
CHEMBL3780629 1 -
CHEMBL3780089 1 -
CHEMBL3782036 1 -
CHEMBL143134 1 -
CHEMBL3780488 1 -
CHEMBL343227 1 -
CHEMBL3781528 1 -
CHEMBL336001 1 -
CHEMBL103667 DORAMAPIMOD 2.0 1 -
CHEMBL3780111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781245 IC50 = 2.0 nM 8.70
CHEMBL3781473 IC50 = 3.0 nM 8.52
CHEMBL3780667 IC50 = 5.0 nM 8.30
CHEMBL3695568 JNJ-49095397 IC50 = 7.0 nM 8.15
CHEMBL3780386 IC50 = 8.0 nM 8.10
CHEMBL3781982 IC50 = 9.0 nM 8.05
CHEMBL3781687 IC50 = 9.0 nM 8.05
CHEMBL3780519 IC50 = 9.0 nM 8.05
CHEMBL3781532 IC50 = 10.0 nM 8.00
CHEMBL3781102 IC50 = 12.0 nM 7.92
CHEMBL3781413 IC50 = 14.0 nM 7.85
CHEMBL3780832 IC50 = 15.0 nM 7.82
CHEMBL3780410 IC50 = 30.0 nM 7.52
CHEMBL3781587 IC50 = 32.0 nM 7.50
CHEMBL3781244 IC50 = 37.0 nM 7.43
CHEMBL3780154 IC50 = 37.0 nM 7.43
CHEMBL3780714 IC50 = 41.0 nM 7.39
CHEMBL3782009 IC50 = 88.0 nM 7.06
CHEMBL3781430 IC50 = 816.0 nM 6.09
CHEMBL3781999 IC50 = 1581.0 nM 5.80
CHEMBL3781982 Emax = 75.0 % -
CHEMBL3781999 Emax = 51.0 % -
CHEMBL103667 DORAMAPIMOD Emax = 56.0 % -
CHEMBL336001 Emax = 28.0 % -
CHEMBL3781528 Emax = 3.0 % -
CHEMBL343227 Emax = -1.0 % -
CHEMBL3780410 Emax = 64.0 % -
CHEMBL3781587 Emax = 71.0 % -
CHEMBL3780111 Emax = 46.0 % -
CHEMBL3781430 Emax = 66.0 % -
CHEMBL3780488 Emax = 46.0 % -
CHEMBL3782036 Emax = 49.0 % -
CHEMBL3780154 Emax = 76.0 % -
CHEMBL3780629 Emax = 39.0 % -
CHEMBL3782009 Emax = 60.0 % -
CHEMBL3780386 Emax = 68.0 % -
CHEMBL3695568 JNJ-49095397 Emax = 88.0 % -
CHEMBL3780832 Emax = 92.0 % -
CHEMBL143134 Emax = 45.0 % -
CHEMBL3780519 Emax = 80.0 % -
CHEMBL3781687 Emax = 90.0 % -
CHEMBL3781244 Emax = 94.0 % -
CHEMBL3781102 Emax = 101.0 % -
CHEMBL3781473 Emax = 74.0 % -
CHEMBL3780667 Emax = 87.0 % -
CHEMBL3781532 Emax = 76.0 % -
CHEMBL3781245 Emax = 103.0 % -
CHEMBL3781413 Emax = 63.0 % -
CHEMBL3780089 Emax = 47.0 % -
CHEMBL3780714 Emax = 65.0 % -