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Assay Detail

CHEMBL868608

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

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

Assay Information

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

Target

Homo sapiens (CHEMBL372) ↗
Type ORGANISM
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 6.32 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212968 — — 1 7.20
CHEMBL212382 — — 1 7.12
CHEMBL384795 — — 1 7.11
CHEMBL213159 — — 1 7.05
CHEMBL214198 — — 1 6.75
CHEMBL212238 — — 1 6.72
CHEMBL212708 — — 1 6.66
CHEMBL211628 — — 1 6.61
CHEMBL379866 — — 1 6.59
CHEMBL213423 — — 1 6.58
CHEMBL380030 — — 1 6.58
CHEMBL215858 — — 1 6.58
CHEMBL215899 — — 1 6.58
CHEMBL214152 — — 1 6.53
CHEMBL377757 — — 1 6.45
CHEMBL377319 — — 1 6.42
CHEMBL215652 — — 1 6.42
CHEMBL379394 — — 1 6.33
CHEMBL212239 — — 1 6.26
CHEMBL212341 — — 1 6.25
CHEMBL379590 — — 1 6.22
CHEMBL378934 — — 1 6.20
CHEMBL210060 — — 1 6.19
CHEMBL209644 — — 1 6.16
CHEMBL194322 — — 1 6.16
CHEMBL378919 — — 1 6.06
CHEMBL213451 — — 1 6.06
CHEMBL212898 — — 1 6.04
CHEMBL212294 — — 1 6.03
CHEMBL386807 — — 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212968 — IC50 = 63.0 nM 7.20
CHEMBL212382 — IC50 = 76.0 nM 7.12
CHEMBL384795 — IC50 = 77.0 nM 7.11
CHEMBL213159 — IC50 = 90.0 nM 7.05
CHEMBL214198 — IC50 = 180.0 nM 6.75
CHEMBL212238 — IC50 = 190.0 nM 6.72
CHEMBL212708 — IC50 = 220.0 nM 6.66
CHEMBL211628 — IC50 = 245.0 nM 6.61
CHEMBL379866 — IC50 = 259.0 nM 6.59
CHEMBL213423 — IC50 = 263.0 nM 6.58
CHEMBL380030 — IC50 = 265.0 nM 6.58
CHEMBL215858 — IC50 = 260.0 nM 6.58
CHEMBL215899 — IC50 = 263.0 nM 6.58
CHEMBL214152 — IC50 = 297.0 nM 6.53
CHEMBL377757 — IC50 = 353.0 nM 6.45
CHEMBL377319 — IC50 = 385.0 nM 6.42
CHEMBL215652 — IC50 = 380.0 nM 6.42
CHEMBL379394 — IC50 = 470.0 nM 6.33
CHEMBL212239 — IC50 = 550.0 nM 6.26
CHEMBL212341 — IC50 = 565.0 nM 6.25
CHEMBL379590 — IC50 = 600.0 nM 6.22
CHEMBL378934 — IC50 = 631.0 nM 6.20
CHEMBL210060 — IC50 = 650.0 nM 6.19
CHEMBL209644 — IC50 = 697.0 nM 6.16
CHEMBL194322 — IC50 = 685.0 nM 6.16
CHEMBL378919 — IC50 = 873.0 nM 6.06
CHEMBL213451 — IC50 = 865.0 nM 6.06
CHEMBL212898 — IC50 = 910.0 nM 6.04
CHEMBL212294 — IC50 = 937.0 nM 6.03
CHEMBL386807 — IC50 = 935.0 nM 6.03
CHEMBL379929 — IC50 = 973.0 nM 6.01
CHEMBL377606 — IC50 = 1395.0 nM 5.86
CHEMBL214114 — IC50 = 1400.0 nM 5.85
CHEMBL211919 — IC50 = 1553.0 nM 5.81
CHEMBL211735 — IC50 = 1707.0 nM 5.77
CHEMBL211679 — IC50 = 4650.0 nM 5.33
CHEMBL379783 — IC50 = 5350.0 nM 5.27
CHEMBL213501 — IC50 - — -
CHEMBL384117 — IC50 - — -
CHEMBL213258 — IC50 - — -
CHEMBL211362 — IC50 - — -
CHEMBL212038 — IC50 - — -
CHEMBL378752 — IC50 - — -
CHEMBL384967 — IC50 - — -
CHEMBL213374 — IC50 - — -
CHEMBL379112 — IC50 - — -
CHEMBL385352 — IC50 - — -
CHEMBL211151 — IC50 - — -
CHEMBL386360 — IC50 - — -
CHEMBL378328 — IC50 - — -