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Assay Detail

CHEMBL1013116

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

Functional
Inhibition of TNFalpha release in human whole blood
95
Total Activities
95
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 95 5.25 6.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481765 1 6.78
CHEMBL480962 1 6.70
CHEMBL480958 1 6.62
CHEMBL493669 1 6.46
CHEMBL482086 1 6.44
CHEMBL516607 1 6.41
CHEMBL521091 1 6.38
CHEMBL519621 1 6.36
CHEMBL521250 1 6.36
CHEMBL482087 1 6.34
CHEMBL480952 1 6.29
CHEMBL516460 1 6.24
CHEMBL481919 1 6.21
CHEMBL494666 1 6.17
CHEMBL481100 1 6.17
CHEMBL481766 1 6.16
CHEMBL481116 1 5.97
CHEMBL111456 1 5.96
CHEMBL481952 1 5.78
CHEMBL481749 1 5.78
CHEMBL479991 1 5.77
CHEMBL480951 1 5.69
CHEMBL10 SB-203580 1 5.64
CHEMBL479810 1 5.61
CHEMBL494871 1 5.57
CHEMBL494879 1 5.55
CHEMBL482111 1 5.53
CHEMBL324977 1 5.52
CHEMBL481913 1 5.48
CHEMBL481943 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481765 IC50 = 167.0 nM 6.78
CHEMBL480962 IC50 = 201.0 nM 6.70
CHEMBL480958 IC50 = 239.0 nM 6.62
CHEMBL493669 IC50 = 350.0 nM 6.46
CHEMBL482086 IC50 = 362.0 nM 6.44
CHEMBL516607 IC50 = 386.0 nM 6.41
CHEMBL521091 IC50 = 416.0 nM 6.38
CHEMBL519621 IC50 = 435.0 nM 6.36
CHEMBL521250 IC50 = 439.0 nM 6.36
CHEMBL482087 IC50 = 458.0 nM 6.34
CHEMBL480952 IC50 = 515.0 nM 6.29
CHEMBL516460 IC50 = 580.0 nM 6.24
CHEMBL481919 IC50 = 622.0 nM 6.21
CHEMBL481100 IC50 = 680.0 nM 6.17
CHEMBL494666 IC50 = 672.0 nM 6.17
CHEMBL481766 IC50 = 700.0 nM 6.16
CHEMBL481116 IC50 = 1060.0 nM 5.97
CHEMBL111456 IC50 = 1100.0 nM 5.96
CHEMBL481952 IC50 = 1650.0 nM 5.78
CHEMBL481749 IC50 = 1680.0 nM 5.78
CHEMBL479991 IC50 = 1710.0 nM 5.77
CHEMBL480951 IC50 = 2040.0 nM 5.69
CHEMBL10 SB-203580 IC50 = 2300.0 nM 5.64
CHEMBL479810 IC50 = 2430.0 nM 5.61
CHEMBL494871 IC50 = 2670.0 nM 5.57
CHEMBL494879 IC50 = 2810.0 nM 5.55
CHEMBL482111 IC50 = 2930.0 nM 5.53
CHEMBL324977 IC50 = 3000.0 nM 5.52
CHEMBL481913 IC50 = 3300.0 nM 5.48
CHEMBL481943 IC50 = 3570.0 nM 5.45
CHEMBL481750 IC50 = 3680.0 nM 5.43
CHEMBL523880 IC50 = 3930.0 nM 5.41
CHEMBL518964 IC50 = 3990.0 nM 5.40
CHEMBL481883 IC50 = 4320.0 nM 5.37
CHEMBL111364 IC50 = 4330.0 nM 5.36
CHEMBL481926 IC50 = 4540.0 nM 5.34
CHEMBL482279 IC50 = 4640.0 nM 5.33
CHEMBL452471 IC50 = 4880.0 nM 5.31
CHEMBL519628 IC50 = 5190.0 nM 5.29
CHEMBL109352 IC50 = 5100.0 nM 5.29
CHEMBL481918 IC50 = 5400.0 nM 5.27
CHEMBL481882 IC50 = 5520.0 nM 5.26
CHEMBL481944 IC50 = 5880.0 nM 5.23
CHEMBL481912 IC50 = 5940.0 nM 5.23
CHEMBL506320 IC50 = 6220.0 nM 5.21
CHEMBL481950 IC50 = 6380.0 nM 5.20
CHEMBL519624 IC50 = 7430.0 nM 5.13
CHEMBL113419 IC50 = 8650.0 nM 5.06
CHEMBL479998 IC50 = 9860.0 nM 5.01
CHEMBL482112 IC50 = 9850.0 nM 5.01