Assay Detail
Binding
CHEMBL5679003
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FTase in human DLD-1 cells expressing moderate level of P-gp1 using Ras as substrate assessed as inhibition of substrate post-translation processing in presence of 10% human serum by immunoblot analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | DLD-1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.37 | 9.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4586794 | ABT-100 | — | 1 | 9.40 |
| CHEMBL289228 | TIPIFARNIB | 3.0 | 1 | 8.51 |
| CHEMBL351706 | BMS-214662 | 1.0 | 1 | 7.92 |
| CHEMBL298734 | LONAFARNIB | 4.0 | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4586794 | ABT-100 | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL289228 | TIPIFARNIB | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL351706 | BMS-214662 | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL298734 | LONAFARNIB | EC50 | = | 23.0 | nM | 7.64 |