Assay Detail
Binding
CHEMBL686003
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Inhibition of human GGTase-catalyzed incorporation of [3H]GGPP into biotinylated peptide of C-terminal of human K-Ras
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Geranylgeranyl transferase type-1 subunit beta (CHEMBL4135) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.51 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24271 | — | — | 1 | 8.51 |
| CHEMBL283051 | — | — | 1 | 8.02 |
| CHEMBL24733 | — | — | 1 | 8.00 |
| CHEMBL24554 | — | — | 1 | 7.80 |
| CHEMBL23370 | — | — | 1 | 7.75 |
| CHEMBL23753 | — | — | 1 | 7.40 |
| CHEMBL418018 | — | — | 1 | 7.04 |
| CHEMBL277646 | — | — | 1 | 7.00 |
| CHEMBL282349 | — | — | 1 | 6.68 |
| CHEMBL24822 | — | — | 1 | 6.62 |
| CHEMBL24048 | — | — | 1 | 6.44 |
| CHEMBL24123 | — | — | 1 | 6.37 |
| CHEMBL26068 | — | — | 1 | 6.13 |
| CHEMBL22703 | — | — | 1 | 6.06 |
| CHEMBL23578 | — | — | 1 | 5.96 |
| CHEMBL25621 | — | — | 1 | 5.92 |
| CHEMBL26492 | — | — | 1 | 5.75 |
| CHEMBL24043 | — | — | 1 | 5.62 |
| CHEMBL22702 | — | — | 2 | 5.39 |
| CHEMBL25620 | — | — | 1 | 5.25 |
| CHEMBL24159 | — | — | 1 | 4.08 |
| CHEMBL26511 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24271 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL283051 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL24733 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL24554 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL23370 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL23753 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL418018 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL277646 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL282349 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL24822 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL24048 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL24123 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL26068 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL22703 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL23578 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL25621 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL26492 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL24043 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL22702 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL22702 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL25620 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL24159 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL26511 | — | IC50 | > | 10000.0 | nM | - |