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Assay Detail

CHEMBL1944480

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

Functional
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
31
Total Activities
31
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

Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A, Lewthwaite RA, Mahnke A, Mathias JP, Philip J, Smith RT, Stefaniak MH, Yeadon M, Phillips C.
J Med Chem (2011) 54 : 7797 -7814
PubMed 21888439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.45 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1938753 1 9.10
CHEMBL1938745 1 9.10
CHEMBL1938743 1 9.10
CHEMBL1938736 1 9.10
CHEMBL1938744 1 9.10
CHEMBL1938739 1 8.96
CHEMBL1938747 1 8.96
CHEMBL1938751 1 8.92
CHEMBL1938740 1 8.85
CHEMBL1938761 1 8.82
CHEMBL1938749 1 8.82
CHEMBL1938400 PF-03715455 2.0 1 8.77
CHEMBL1938750 1 8.77
CHEMBL1938754 1 8.74
CHEMBL1938755 1 8.72
CHEMBL1938758 1 8.72
CHEMBL1938737 1 8.70
CHEMBL1938741 1 8.70
CHEMBL1938756 1 8.60
CHEMBL1938746 1 8.57
CHEMBL1938757 1 8.46
CHEMBL1938762 1 8.24
CHEMBL1938738 1 8.17
CHEMBL1938752 1 7.97
CHEMBL1938759 1 7.97
CHEMBL103667 DORAMAPIMOD 2.0 1 7.82
CHEMBL1938760 1 7.66
CHEMBL1938763 1 7.40
CHEMBL1938764 1 7.24
CHEMBL1938742 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1938753 IC50 = 0.8 nM 9.10
CHEMBL1938745 IC50 = 0.8 nM 9.10
CHEMBL1938743 IC50 = 0.8 nM 9.10
CHEMBL1938736 IC50 = 0.8 nM 9.10
CHEMBL1938744 IC50 = 0.8 nM 9.10
CHEMBL1938739 IC50 = 1.1 nM 8.96
CHEMBL1938747 IC50 = 1.1 nM 8.96
CHEMBL1938751 IC50 = 1.2 nM 8.92
CHEMBL1938740 IC50 = 1.4 nM 8.85
CHEMBL1938761 IC50 = 1.5 nM 8.82
CHEMBL1938749 IC50 = 1.5 nM 8.82
CHEMBL1938400 PF-03715455 IC50 = 1.7 nM 8.77
CHEMBL1938750 IC50 = 1.7 nM 8.77
CHEMBL1938754 IC50 = 1.8 nM 8.74
CHEMBL1938755 IC50 = 1.9 nM 8.72
CHEMBL1938758 IC50 = 1.9 nM 8.72
CHEMBL1938737 IC50 = 2.0 nM 8.70
CHEMBL1938741 IC50 = 2.0 nM 8.70
CHEMBL1938756 IC50 = 2.5 nM 8.60
CHEMBL1938746 IC50 = 2.7 nM 8.57
CHEMBL1938757 IC50 = 3.5 nM 8.46
CHEMBL1938762 IC50 = 5.7 nM 8.24
CHEMBL1938738 IC50 = 6.7 nM 8.17
CHEMBL1938752 IC50 = 10.6 nM 7.97
CHEMBL1938759 IC50 = 10.6 nM 7.97
CHEMBL103667 DORAMAPIMOD IC50 = 15.0 nM 7.82
CHEMBL1938760 IC50 = 22.0 nM 7.66
CHEMBL1938763 IC50 = 40.0 nM 7.40
CHEMBL1938764 IC50 = 58.0 nM 7.24
CHEMBL1938742 IC50 = 74.0 nM 7.13
CHEMBL1938748 IC50 = 155.0 nM 6.81