Assay Detail
Binding
CHEMBL680083
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Inhibition of human farnesyltransferase in PSN-1 cells.
32
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | PSN-1 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 | 32 | 8.32 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52073 | — | — | 1 | 10.00 |
| CHEMBL80702 | — | — | 2 | 8.96 |
| CHEMBL498100 | — | — | 1 | 8.92 |
| CHEMBL310586 | — | — | 1 | 8.89 |
| CHEMBL311561 | — | — | 1 | 8.85 |
| CHEMBL77504 | — | — | 1 | 8.85 |
| CHEMBL526521 | — | — | 1 | 8.82 |
| CHEMBL525368 | — | — | 1 | 8.82 |
| CHEMBL496879 | — | — | 1 | 8.80 |
| CHEMBL78742 | — | — | 2 | 8.72 |
| CHEMBL312137 | — | — | 1 | 8.72 |
| CHEMBL523080 | — | — | 1 | 8.68 |
| CHEMBL524082 | — | — | 1 | 8.64 |
| CHEMBL312034 | — | — | 2 | 8.60 |
| CHEMBL279433 | L-778123 FREE BASE | 1.0 | 1 | 8.48 |
| CHEMBL502560 | — | — | 1 | 8.46 |
| CHEMBL53821 | — | — | 1 | 8.46 |
| CHEMBL526656 | — | — | 1 | 8.44 |
| CHEMBL312121 | — | — | 1 | 8.31 |
| CHEMBL465417 | — | — | 1 | 8.31 |
| CHEMBL310943 | — | — | 2 | 8.00 |
| CHEMBL312459 | — | — | 1 | 7.64 |
| CHEMBL523570 | — | — | 1 | 7.36 |
| CHEMBL524909 | — | — | 1 | 7.27 |
| CHEMBL498101 | — | — | 1 | 5.75 |
| 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 | - |
| CHEMBL516874 | — | — | 1 | - |
| CHEMBL526466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52073 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL80702 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL80702 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL498100 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL310586 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL311561 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL77504 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL525368 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL526521 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL496879 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL312137 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL78742 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL523080 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL524082 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL312034 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL279433 | L-778123 FREE BASE | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL53821 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL502560 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL526656 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL465417 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL312121 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL310943 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL312459 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL312034 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL523570 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL524909 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL310943 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL78742 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL498101 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL516874 | — | IC50 | < | 1.0 | nM | - |
| 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 | < | 1.0 | nM | - |
| CHEMBL526466 | — | IC50 | < | 1.0 | nM | - |