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Assay Detail

CHEMBL1025675

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Functional
Inhibition of TNF-alpha-induced IL8 production in human whole blood cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Herberich B, Cao GQ, Chakrabarti PP, Falsey JR, Pettus L, Rzasa RM, Reed AB, Reichelt A, Sham K, Thaman M, Wurz RP, Xu S, Zhang D, Hsieh F, Lee MR, Syed R, Li V, Grosfeld D, Plant MH, Henkle B, Sherman L, Middleton S, Wong LM, Tasker AS.
J Med Chem (2008) 51 : 6271 -6279
PubMed 18817365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.54 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494272 1 9.05
CHEMBL494469 1 8.92
CHEMBL493670 1 8.80
CHEMBL492265 1 8.60
CHEMBL493671 1 8.57
CHEMBL495330 1 8.46
CHEMBL494270 1 8.37
CHEMBL493708 1 8.09
CHEMBL494072 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494272 IC50 = 0.9 nM 9.05
CHEMBL494469 IC50 = 1.2 nM 8.92
CHEMBL493670 IC50 = 1.6 nM 8.80
CHEMBL492265 IC50 = 2.5 nM 8.60
CHEMBL493671 IC50 = 2.7 nM 8.57
CHEMBL495330 IC50 = 3.5 nM 8.46
CHEMBL494270 IC50 = 4.3 nM 8.37
CHEMBL493708 IC50 = 8.1 nM 8.09
CHEMBL494072 IC50 = 10.7 nM 7.97