Assay Detail
Binding
CHEMBL681129
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Inhibition of Farnesyltransferase in cells, evaluated in a radiotracer assay for farnesyltransferase inhibition (CRAFTI), in cultured H-ras-transformed Rat cells
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Protein farnesyltransferase (CHEMBL2095197) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.75 | 10.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310586 | — | — | 1 | 10.49 |
| CHEMBL525369 | (1R,5R)-30-OXO-19-OXA-2,6,10,12-TETRAAZAHEXACYCLO[18.6.2.1^{2,5}.1^{14,18}.0^{8,12}.0^{23,27}]TRIACONTA-8,10,14(29),15,17,20(28),21,23(27)-OCTAENE-17-CARBONITRILE (STRUCTURAL MIX) | — | 1 | 10.27 |
| CHEMBL516874 | — | — | 1 | 10.20 |
| CHEMBL311561 | — | — | 1 | 9.72 |
| CHEMBL525368 | — | — | 1 | 9.68 |
| CHEMBL526521 | — | — | 1 | 9.68 |
| CHEMBL526466 | — | — | 1 | 9.66 |
| CHEMBL52073 | — | — | 1 | 9.54 |
| CHEMBL80702 | — | — | 2 | 9.49 |
| CHEMBL312137 | — | — | 1 | 9.28 |
| CHEMBL498100 | — | — | 1 | 9.24 |
| CHEMBL77504 | — | — | 1 | 9.19 |
| CHEMBL502560 | — | — | 1 | 9.18 |
| CHEMBL78742 | — | — | 2 | 9.06 |
| CHEMBL465417 | — | — | 1 | 8.74 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 8.44 |
| CHEMBL53821 | — | — | 1 | 8.42 |
| CHEMBL496879 | — | — | 1 | 8.36 |
| CHEMBL523080 | — | — | 1 | 8.17 |
| CHEMBL524082 | — | — | 1 | 7.89 |
| CHEMBL312121 | — | — | 1 | 7.41 |
| CHEMBL526656 | — | — | 1 | 7.39 |
| CHEMBL523570 | — | — | 1 | 7.03 |
| CHEMBL312034 | — | — | 1 | 6.70 |
| CHEMBL310943 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310586 | — | IC50 | = | 0.032 | nM | 10.49 |
| CHEMBL525369 | (1R,5R)-30-OXO-19-OXA-2,6,10,12-TETRAAZAHEXACYCLO[18.6.2.1^{2,5}.1^{14,18}.0^{8,12}.0^{23,27}]TRIACONTA-8,10,14(29),15,17,20(28),21,23(27)-OCTAENE-17-CARBONITRILE (STRUCTURAL MIX) | IC50 | = | 0.054 | nM | 10.27 |
| CHEMBL516874 | — | IC50 | = | 0.063 | nM | 10.20 |
| CHEMBL311561 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL525368 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL526521 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL526466 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL52073 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL80702 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL80702 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL312137 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL498100 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL77504 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL502560 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL78742 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL465417 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL53821 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL496879 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL523080 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL524082 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL312121 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL526656 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL78742 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL523570 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL312034 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL310943 | — | IC50 | = | 230.0 | nM | 6.64 |