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Assay Detail

CHEMBL867926

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

Functional
Inhibition of LPS-induced TNFalpha production in human monocytes
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Monocyte
Confidence 1 — Organism
Curated By Expert

Target

Monocyte (CHEMBL614076)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.
McClure KF, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F.
Bioorg Med Chem Lett (2006) 16 : 4339 -4344
PubMed 16759861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 76 7.27 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212968 1 8.08
CHEMBL384795 1 8.00
CHEMBL209644 1 8.00
CHEMBL213258 1 8.00
CHEMBL213159 1 8.00
CHEMBL378919 1 8.00
CHEMBL380030 1 8.00
CHEMBL212238 1 8.00
CHEMBL439321 1 8.00
CHEMBL215858 1 7.94
CHEMBL212382 1 7.90
CHEMBL214198 1 7.85
CHEMBL212708 1 7.85
CHEMBL213423 1 7.71
CHEMBL379590 1 7.70
CHEMBL377875 1 7.61
CHEMBL214152 1 7.61
CHEMBL215652 1 7.61
CHEMBL379866 1 7.60
CHEMBL215899 1 7.55
CHEMBL211628 1 7.52
CHEMBL211362 1 7.52
CHEMBL212849 1 7.50
CHEMBL214114 1 7.50
CHEMBL211919 1 7.46
CHEMBL379394 1 7.41
CHEMBL379374 1 7.40
CHEMBL211735 1 7.40
CHEMBL212341 1 7.40
CHEMBL386360 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212968 IC50 = 8.3 nM 8.08
CHEMBL384795 IC50 = 10.0 nM 8.00
CHEMBL209644 IC50 = 10.0 nM 8.00
CHEMBL213258 IC50 = 10.0 nM 8.00
CHEMBL213159 IC50 = 10.0 nM 8.00
CHEMBL380030 IC50 = 10.0 nM 8.00
CHEMBL212238 IC50 = 10.0 nM 8.00
CHEMBL439321 IC50 = 10.0 nM 8.00
CHEMBL378919 IC50 = 10.0 nM 8.00
CHEMBL215858 IC50 = 11.6 nM 7.94
CHEMBL212382 IC50 = 12.6 nM 7.90
CHEMBL214198 IC50 = 14.1 nM 7.85
CHEMBL212708 IC50 = 14.1 nM 7.85
CHEMBL213423 IC50 = 19.7 nM 7.71
CHEMBL379590 IC50 = 20.0 nM 7.70
CHEMBL377875 IC50 = 24.5 nM 7.61
CHEMBL214152 IC50 = 24.5 nM 7.61
CHEMBL215652 IC50 = 24.5 nM 7.61
CHEMBL379866 IC50 = 25.0 nM 7.60
CHEMBL215899 IC50 = 28.3 nM 7.55
CHEMBL211628 IC50 = 30.0 nM 7.52
CHEMBL211362 IC50 = 30.0 nM 7.52
CHEMBL212849 IC50 = 31.6 nM 7.50
CHEMBL214114 IC50 = 31.6 nM 7.50
CHEMBL211919 IC50 = 34.6 nM 7.46
CHEMBL379394 IC50 = 38.7 nM 7.41
CHEMBL211735 IC50 = 40.0 nM 7.40
CHEMBL212341 IC50 = 40.0 nM 7.40
CHEMBL386360 IC50 = 40.0 nM 7.40
CHEMBL379374 IC50 = 40.0 nM 7.40
CHEMBL212898 IC50 = 45.8 nM 7.34
CHEMBL377319 IC50 = 45.8 nM 7.34
CHEMBL194322 IC50 = 45.3 nM 7.34
CHEMBL378934 IC50 = 47.2 nM 7.33
CHEMBL211678 IC50 = 49.0 nM 7.31
CHEMBL378752 IC50 = 49.0 nM 7.31
CHEMBL377757 IC50 = 50.0 nM 7.30
CHEMBL213451 IC50 = 52.0 nM 7.28
CHEMBL386807 IC50 = 52.0 nM 7.28
CHEMBL212239 IC50 = 52.3 nM 7.28
CHEMBL213598 IC50 = 54.8 nM 7.26
CHEMBL385352 IC50 = 57.4 nM 7.24
CHEMBL378697 IC50 = 57.4 nM 7.24
CHEMBL212294 IC50 = 57.4 nM 7.24
CHEMBL214310 IC50 = 60.0 nM 7.22
CHEMBL378920 IC50 = 60.0 nM 7.22
CHEMBL210060 IC50 = 60.0 nM 7.22
CHEMBL386033 IC50 = 63.0 nM 7.20
CHEMBL377538 IC50 = 69.3 nM 7.16
CHEMBL212655 IC50 = 70.0 nM 7.16