Assay Detail
Binding
CHEMBL2405979
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Inhibition of human p38alpha expressed in Escherichia coli using MBP as substrate preincubated for 10 mins prior to substrate addition measured after 45 mins by microbeta scintillation counting analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.17 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2401994 | — | — | 1 | 9.70 |
| CHEMBL2401995 | — | — | 1 | 9.10 |
| CHEMBL2401981 | — | — | 1 | 8.70 |
| CHEMBL2402000 | — | — | 1 | 8.55 |
| CHEMBL2401985 | — | — | 1 | 8.42 |
| CHEMBL2401993 | — | — | 1 | 8.42 |
| CHEMBL258202 | — | — | 1 | 8.40 |
| CHEMBL2401979 | — | — | 1 | 8.40 |
| CHEMBL2401988 | — | — | 1 | 8.40 |
| CHEMBL2401987 | — | — | 1 | 8.39 |
| CHEMBL2401989 | — | — | 1 | 8.39 |
| CHEMBL2401983 | — | — | 1 | 8.32 |
| CHEMBL2401990 | — | — | 1 | 8.30 |
| CHEMBL2401991 | — | — | 1 | 8.27 |
| CHEMBL2401978 | — | — | 1 | 8.15 |
| CHEMBL2401999 | — | — | 1 | 8.11 |
| CHEMBL2402001 | — | — | 1 | 8.11 |
| CHEMBL2401984 | — | — | 1 | 8.10 |
| CHEMBL2401992 | — | — | 1 | 8.07 |
| CHEMBL2401982 | — | — | 1 | 8.05 |
| CHEMBL2401998 | — | — | 1 | 7.96 |
| CHEMBL2401997 | — | — | 1 | 7.89 |
| CHEMBL2401986 | — | — | 1 | 7.85 |
| CHEMBL2402005 | — | — | 1 | 7.64 |
| CHEMBL2402002 | — | — | 1 | 7.50 |
| CHEMBL2402004 | — | — | 1 | 7.47 |
| CHEMBL2402003 | — | — | 1 | 7.46 |
| CHEMBL2401996 | — | — | 1 | 7.39 |
| CHEMBL2401980 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2401994 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2401995 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2401981 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2402000 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2401985 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2401993 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL258202 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2401979 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2401988 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2401987 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2401989 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2401983 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2401990 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2401991 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2401978 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2401999 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2402001 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2401984 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2401992 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2401982 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2401998 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2401997 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2401986 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2402005 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2402002 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2402004 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2402003 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2401996 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2401980 | — | IC50 | = | 46.0 | nM | 7.34 |