Assay Detail
Binding
CHEMBL685883
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Inhibition of rate of incorporation of [3H]GGPP into a biotinylated peptide corresponding to C-terminus of human Ki-Ras by human geranylgeranyl-transferase type I.
37
Total Activities
37
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
Diaryl ether inhibitors of farnesyl-protein transferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.76 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282499 | — | — | 1 | 8.15 |
| CHEMBL22659 | — | — | 1 | 7.64 |
| CHEMBL282001 | — | — | 1 | 6.55 |
| CHEMBL22319 | — | — | 1 | 6.55 |
| CHEMBL22800 | — | — | 1 | 6.42 |
| CHEMBL22819 | — | — | 1 | 6.28 |
| CHEMBL22959 | — | — | 1 | 6.28 |
| CHEMBL22710 | — | — | 1 | 6.28 |
| CHEMBL24985 | — | — | 1 | 6.22 |
| CHEMBL25606 | — | — | 1 | 6.20 |
| CHEMBL22718 | — | — | 1 | 6.13 |
| CHEMBL22440 | — | — | 1 | 6.08 |
| CHEMBL25542 | — | — | 1 | 6.04 |
| CHEMBL22235 | — | — | 1 | 5.96 |
| CHEMBL25500 | — | — | 1 | 5.92 |
| CHEMBL279923 | — | — | 1 | 5.89 |
| CHEMBL423109 | — | — | 1 | 5.70 |
| CHEMBL280384 | — | — | 1 | 5.70 |
| CHEMBL22080 | — | — | 1 | 5.58 |
| CHEMBL23019 | — | — | 1 | 5.54 |
| CHEMBL22568 | — | — | 1 | 5.51 |
| CHEMBL277489 | — | — | 1 | 5.50 |
| CHEMBL22847 | — | — | 1 | 5.50 |
| CHEMBL25439 | — | — | 1 | 5.48 |
| CHEMBL279066 | — | — | 1 | 5.46 |
| CHEMBL22826 | — | — | 1 | 5.46 |
| CHEMBL25602 | — | — | 1 | 5.43 |
| CHEMBL280905 | — | — | 1 | 5.36 |
| CHEMBL25217 | — | — | 1 | 5.21 |
| CHEMBL283323 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282499 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL22659 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL22319 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL282001 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL22800 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL22819 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL22959 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL22710 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL24985 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL25606 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL22718 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL22440 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL25542 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL22235 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL25500 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL279923 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL423109 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL280384 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL22080 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL23019 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL22568 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL277489 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL22847 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL25439 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL279066 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL22826 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL25602 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL280905 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL25217 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL283323 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL22454 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL22238 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL22547 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL24888 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL23011 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL22854 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL25550 | — | IC50 | = | 28000.0 | nM | 4.55 |