Assay Detail
Binding
CHEMBL683539
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Inhibition of Geranylgeranylprotein transferase-I catalyzed incorporation of [3H]GGPP into biotinYRASNRSCAIL peptide
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.30 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337751 | — | — | 2 | 7.09 |
| CHEMBL341586 | — | — | 2 | 6.34 |
| CHEMBL289228 | TIPIFARNIB | 3.0 | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337751 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL337751 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL341586 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL289228 | TIPIFARNIB | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL341586 | — | IC50 | > | 1000.0 | nM | - |