Assay Detail
Binding
CHEMBL683658
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Concentration required to inhibit recombinant human geranylgeranyl transferase type I (GGTase-I) catalyzed incorporation of [3H]GGPP to the C-terminus of human K-Ras.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Geranylgeranyl transferase type I (CHEMBL2095164) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.76 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL322435 | — | — | 1 | 9.09 |
| CHEMBL99901 | — | — | 1 | 8.85 |
| CHEMBL450336 | — | — | 1 | 8.68 |
| CHEMBL316673 | — | — | 1 | 8.60 |
| CHEMBL318626 | — | — | 1 | 8.54 |
| CHEMBL294888 | — | — | 1 | 8.44 |
| CHEMBL2111612 | — | — | 1 | 8.35 |
| CHEMBL102293 | — | — | 1 | 8.29 |
| CHEMBL1907916 | — | — | 1 | 8.24 |
| CHEMBL282499 | — | — | 1 | 8.14 |
| CHEMBL329932 | — | — | 1 | 8.10 |
| CHEMBL415246 | — | — | 1 | 8.05 |
| CHEMBL100526 | — | — | 1 | 8.00 |
| CHEMBL103357 | — | — | 1 | 7.92 |
| CHEMBL319427 | — | — | 1 | 7.89 |
| CHEMBL439047 | — | — | 1 | 7.89 |
| CHEMBL420273 | — | — | 1 | 7.77 |
| CHEMBL321796 | — | — | 1 | 7.70 |
| CHEMBL2092921 | — | — | 1 | 7.60 |
| CHEMBL323302 | — | — | 1 | 7.52 |
| CHEMBL400694 | — | — | 1 | 7.27 |
| CHEMBL320425 | — | — | 1 | 7.04 |
| CHEMBL320892 | — | — | 1 | 6.55 |
| CHEMBL318923 | — | — | 1 | 6.25 |
| CHEMBL100868 | — | — | 1 | 5.92 |
| CHEMBL103625 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL322435 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL99901 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL450336 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL316673 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL318626 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL294888 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2111612 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL102293 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1907916 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL282499 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL329932 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL415246 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL100526 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL103357 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL319427 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL439047 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL420273 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL321796 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2092921 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL323302 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL400694 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL320425 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL320892 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL318923 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL100868 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL103625 | — | IC50 | = | 10000.0 | nM | 5.00 |