Assay Detail
Binding
CHEMBL4056784
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Inhibition of recombinant human farnesyltransferase using dansyl-GCVLS as substrate in presence of farnesyl pyrophosphate after 15 mins by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.08 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54044 | — | — | 1 | 7.82 |
| CHEMBL4066468 | — | — | 1 | 7.27 |
| CHEMBL4087793 | — | — | 1 | 6.85 |
| CHEMBL4076843 | — | — | 1 | 6.77 |
| CHEMBL4086502 | — | — | 1 | 6.35 |
| CHEMBL4079913 | — | — | 1 | 6.11 |
| CHEMBL4096919 | — | — | 1 | 6.00 |
| CHEMBL4104149 | — | — | 1 | 5.91 |
| CHEMBL4104673 | — | — | 1 | 5.82 |
| CHEMBL4090877 | — | — | 1 | 5.77 |
| CHEMBL4098096 | — | — | 1 | 5.51 |
| CHEMBL4105597 | — | — | 1 | 5.33 |
| CHEMBL4075066 | — | — | 1 | 4.83 |
| CHEMBL4095500 | — | — | 1 | 4.76 |
| CHEMBL4075495 | — | — | 1 | - |
| CHEMBL4063801 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54044 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4066468 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4087793 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4076843 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4086502 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4079913 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4096919 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4104149 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4104673 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4090877 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4098096 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4105597 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4075066 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4095500 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL4075495 | — | IC50 | > | 22000.0 | nM | - |
| CHEMBL4063801 | — | IC50 | > | 22300.0 | nM | - |