Assay Detail
Binding
CHEMBL768930
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Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val
14
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | monkey |
| Cell Type | kidney |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.90 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298734 | LONAFARNIB | 4.0 | 1 | 8.72 |
| CHEMBL333864 | — | — | 1 | 8.70 |
| CHEMBL127697 | — | — | 1 | 8.59 |
| CHEMBL338930 | — | — | 1 | 8.24 |
| CHEMBL125101 | — | — | 2 | 8.13 |
| CHEMBL340432 | — | — | 1 | 7.72 |
| CHEMBL126913 | — | — | 1 | 7.47 |
| CHEMBL127860 | — | — | 1 | 7.38 |
| CHEMBL339026 | — | — | 2 | 7.19 |
| CHEMBL126423 | — | — | 2 | 7.16 |
| CHEMBL125344 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298734 | LONAFARNIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL333864 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL127697 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL338930 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL125101 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL340432 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL125101 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL126913 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL127860 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL339026 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL126423 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL125344 | — | IC50 | > | 190.0 | nM | - |
| CHEMBL126423 | — | IC50 | > | 180.0 | nM | - |
| CHEMBL339026 | — | IC50 | > | 190.0 | nM | - |