Assay Detail
Binding
CHEMBL4199514
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Inhibition of recombinant human sPLA2-10 using human HDL as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assay
24
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of Selective sPLA2-X Inhibitor (-)-2-{2-[Carbamoyl-6-(trifluoromethoxy)-1H-indol-1-yl]pyridine-2-yl}propanoic Acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.38 | 7.38 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215835 | — | — | 3 | 7.38 |
| CHEMBL4210991 | — | — | 1 | 6.96 |
| CHEMBL4204172 | — | — | 2 | 6.85 |
| CHEMBL4217510 | — | — | 1 | 6.60 |
| CHEMBL4205511 | — | — | 2 | 6.60 |
| CHEMBL4171084 | — | — | 1 | 6.51 |
| CHEMBL4203027 | — | — | 2 | 6.48 |
| CHEMBL4214052 | — | — | 2 | 6.46 |
| CHEMBL4213094 | — | — | 1 | 6.19 |
| CHEMBL4205008 | — | — | 2 | 6.08 |
| CHEMBL4206163 | — | — | 1 | 5.80 |
| CHEMBL4204160 | — | — | 1 | - |
| CHEMBL4207266 | — | — | 1 | - |
| CHEMBL4207065 | — | — | 1 | - |
| CHEMBL4213633 | — | — | 1 | - |
| CHEMBL4204365 | — | — | 1 | - |
| CHEMBL4209236 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215835 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4210991 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4204172 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4205511 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4217510 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4171084 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4203027 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4214052 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4213094 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4205008 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4206163 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4214052 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4205008 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4215835 | — | IC90 | = | 362.0 | nM | - |
| CHEMBL4204160 | — | IC50 | - | — | - | |
| CHEMBL4203027 | — | IC50 | - | — | - | |
| CHEMBL4205511 | — | IC50 | - | — | - | |
| CHEMBL4215835 | — | IC50 | - | — | - | |
| CHEMBL4207266 | — | IC50 | - | — | - | |
| CHEMBL4204172 | — | IC50 | - | — | - | |
| CHEMBL4207065 | — | IC50 | - | — | - | |
| CHEMBL4213633 | — | IC50 | - | — | - | |
| CHEMBL4204365 | — | IC50 | - | — | - | |
| CHEMBL4209236 | — | IC50 | - | — | - |