Assay Detail
Binding
CHEMBL680087
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Inhibitory activity against Hras Farnesyltransferase (FPT).
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.48 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90435 | — | — | 1 | 9.10 |
| CHEMBL315402 | — | — | 1 | 9.10 |
| CHEMBL443022 | — | — | 1 | 8.74 |
| CHEMBL88713 | — | — | 1 | 8.72 |
| CHEMBL298734 | LONAFARNIB | 4.0 | 1 | 8.72 |
| CHEMBL432573 | — | — | 1 | 8.70 |
| CHEMBL423680 | — | — | 1 | 8.70 |
| CHEMBL90050 | — | — | 1 | 8.68 |
| CHEMBL315915 | — | — | 1 | 8.66 |
| CHEMBL89304 | — | — | 1 | 8.57 |
| CHEMBL264305 | — | — | 1 | 8.51 |
| CHEMBL91213 | — | — | 1 | 8.37 |
| CHEMBL88432 | — | — | 1 | 8.28 |
| CHEMBL314996 | — | — | 1 | 8.28 |
| CHEMBL90234 | — | — | 1 | 8.10 |
| CHEMBL328743 | — | — | 1 | 7.77 |
| CHEMBL313350 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90435 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL315402 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL443022 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL88713 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL298734 | LONAFARNIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL432573 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL423680 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL90050 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL315915 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL89304 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL264305 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL91213 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL88432 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL314996 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL90234 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL328743 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL313350 | — | IC50 | = | 76.1 | nM | 7.12 |