Assay Detail
Functional
CHEMBL4353489
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Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.16 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554455 | — | — | 1 | 9.00 |
| CHEMBL4469292 | — | — | 1 | 8.40 |
| CHEMBL4458861 | — | — | 1 | 8.00 |
| CHEMBL4453821 | — | — | 1 | 8.00 |
| CHEMBL4559783 | — | — | 1 | 8.00 |
| CHEMBL4514099 | — | — | 1 | 8.00 |
| CHEMBL4463158 | — | — | 1 | 7.70 |
| CHEMBL4438250 | — | — | 1 | 7.52 |
| CHEMBL4525498 | — | — | 1 | 7.52 |
| CHEMBL4476614 | — | — | 1 | 7.52 |
| CHEMBL4444594 | — | — | 1 | 7.52 |
| CHEMBL4538710 | — | — | 1 | 7.52 |
| CHEMBL4476042 | — | — | 1 | 7.40 |
| CHEMBL4440684 | — | — | 1 | 7.30 |
| CHEMBL4461409 | — | — | 1 | 7.30 |
| CHEMBL4476367 | — | — | 1 | 7.22 |
| CHEMBL4454063 | — | — | 1 | 7.22 |
| CHEMBL4450265 | — | — | 1 | 7.22 |
| CHEMBL4455390 | — | — | 1 | 7.05 |
| CHEMBL4556839 | — | — | 1 | 6.96 |
| CHEMBL4590434 | — | — | 1 | 6.80 |
| CHEMBL4558022 | — | — | 1 | 6.58 |
| CHEMBL458997 | — | — | 1 | 6.54 |
| CHEMBL4453262 | — | — | 1 | 6.36 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.58 |
| CHEMBL4437276 | — | — | 1 | 5.45 |
| CHEMBL4468772 | — | — | 1 | 5.42 |
| CHEMBL4445960 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554455 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4469292 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4458861 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4453821 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4559783 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4514099 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4463158 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4438250 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4525498 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4476614 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4444594 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4538710 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4476042 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4440684 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4461409 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4476367 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4454063 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4450265 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4455390 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4556839 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4590434 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4558022 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL458997 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4453262 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3137331 | DEFACTINIB | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL4437276 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL4468772 | — | IC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL4445960 | — | IC50 | = | 4690.0 | nM | 5.33 |