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Assay Detail

CHEMBL1013117

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

Functional
Inhibition of IL1-beta release in human whole blood
80
Total Activities
80
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

Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
Laufer SA, Hauser DR, Domeyer DM, Kinkel K, Liedtke AJ.
J Med Chem (2008) 51 : 4122 -4149
PubMed 18578517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 5.53 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113419 1 7.36
CHEMBL109352 1 7.10
CHEMBL482087 1 6.87
CHEMBL480952 1 6.60
CHEMBL111456 1 6.42
CHEMBL481765 1 6.20
CHEMBL482279 1 5.89
CHEMBL482111 1 5.87
CHEMBL521091 1 5.72
CHEMBL10 SB-203580 1 5.70
CHEMBL493669 1 5.62
CHEMBL481919 1 5.56
CHEMBL324977 1 5.39
CHEMBL111364 1 5.36
CHEMBL518964 1 5.12
CHEMBL494666 1 5.12
CHEMBL523880 1 5.00
CHEMBL481706 1 4.99
CHEMBL494879 1 4.79
CHEMBL519617 1 4.63
CHEMBL480957 1 4.56
CHEMBL494901 1 4.46
CHEMBL481965 1 4.23
CHEMBL516761 1 4.21
CHEMBL109028 1 -
CHEMBL481116 1 -
CHEMBL452471 1 -
CHEMBL479416 1 -
CHEMBL481316 1 -
CHEMBL481315 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113419 IC50 = 44.0 nM 7.36
CHEMBL109352 IC50 = 80.0 nM 7.10
CHEMBL482087 IC50 = 136.0 nM 6.87
CHEMBL480952 IC50 = 250.0 nM 6.60
CHEMBL111456 IC50 = 380.0 nM 6.42
CHEMBL481765 IC50 = 630.0 nM 6.20
CHEMBL482279 IC50 = 1290.0 nM 5.89
CHEMBL482111 IC50 = 1360.0 nM 5.87
CHEMBL521091 IC50 = 1890.0 nM 5.72
CHEMBL10 SB-203580 IC50 = 1980.0 nM 5.70
CHEMBL493669 IC50 = 2370.0 nM 5.62
CHEMBL481919 IC50 = 2760.0 nM 5.56
CHEMBL324977 IC50 = 4100.0 nM 5.39
CHEMBL111364 IC50 = 4330.0 nM 5.36
CHEMBL494666 IC50 = 7640.0 nM 5.12
CHEMBL518964 IC50 = 7560.0 nM 5.12
CHEMBL523880 IC50 = 10100.0 nM 5.00
CHEMBL481706 IC50 = 10300.0 nM 4.99
CHEMBL494879 IC50 = 16200.0 nM 4.79
CHEMBL519617 IC50 = 23500.0 nM 4.63
CHEMBL480957 IC50 = 27400.0 nM 4.56
CHEMBL494901 IC50 = 35000.0 nM 4.46
CHEMBL481965 IC50 = 59300.0 nM 4.23
CHEMBL516761 IC50 = 61300.0 nM 4.21
CHEMBL480956 IC50 - -
CHEMBL481698 IC50 - -
CHEMBL522362 IC50 - -
CHEMBL494665 IC50 - -
CHEMBL524015 IC50 - -
CHEMBL109383 IC50 - -
CHEMBL521692 IC50 - -
CHEMBL110262 IC50 - -
CHEMBL494902 IC50 - -
CHEMBL481945 IC50 - -
CHEMBL113060 IC50 - -
CHEMBL111403 IC50 - -
CHEMBL481751 IC50 - -
CHEMBL479985 IC50 - -
CHEMBL494871 IC50 - -
CHEMBL516607 IC50 - -
CHEMBL480962 IC50 - -
CHEMBL481100 IC50 - -
CHEMBL493870 IC50 - -
CHEMBL518962 IC50 - -
CHEMBL481315 IC50 - -
CHEMBL481316 IC50 - -
CHEMBL479416 IC50 - -
CHEMBL452471 IC50 - -
CHEMBL481116 IC50 - -
CHEMBL109028 IC50 - -