Assay Detail
Functional
CHEMBL4730122
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Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.57 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4776012 | — | — | 1 | 6.85 |
| CHEMBL4785849 | — | — | 1 | 6.21 |
| CHEMBL4740234 | — | — | 1 | 6.06 |
| CHEMBL4742222 | — | — | 1 | 5.97 |
| CHEMBL4780830 | — | — | 1 | 5.94 |
| CHEMBL4745868 | — | — | 1 | 5.89 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.85 |
| CHEMBL4764242 | — | — | 1 | 5.83 |
| CHEMBL4741781 | — | — | 1 | 5.80 |
| CHEMBL4776073 | — | — | 1 | 5.74 |
| CHEMBL4779604 | — | — | 1 | 5.72 |
| CHEMBL4786175 | — | — | 1 | 5.66 |
| CHEMBL4785358 | — | — | 1 | 5.62 |
| CHEMBL4764869 | — | — | 1 | 5.54 |
| CHEMBL4793105 | — | — | 1 | 5.50 |
| CHEMBL4746377 | — | — | 1 | 5.43 |
| CHEMBL4744921 | — | — | 1 | 5.35 |
| CHEMBL4789716 | — | — | 1 | 5.27 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 5.22 |
| CHEMBL4777979 | — | — | 1 | 5.21 |
| CHEMBL4794857 | — | — | 1 | 5.19 |
| CHEMBL4781919 | — | — | 1 | 5.15 |
| CHEMBL4787381 | — | — | 1 | 5.15 |
| CHEMBL4791607 | — | — | 1 | 4.97 |
| CHEMBL4800037 | — | — | 1 | 4.96 |
| CHEMBL4795593 | — | — | 1 | 4.74 |
| CHEMBL4758137 | — | — | 1 | - |
| CHEMBL4748415 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4776012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4785849 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4740234 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4742222 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4780830 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL4745868 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4764242 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4741781 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL4776073 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4779604 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL4786175 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4785358 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL4764869 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL4793105 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL4746377 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL4744921 | — | IC50 | = | 4440.0 | nM | 5.35 |
| CHEMBL4789716 | — | IC50 | = | 5370.0 | nM | 5.27 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 6010.0 | nM | 5.22 |
| CHEMBL4777979 | — | IC50 | = | 6160.0 | nM | 5.21 |
| CHEMBL4794857 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4781919 | — | IC50 | = | 7090.0 | nM | 5.15 |
| CHEMBL4787381 | — | IC50 | = | 7130.0 | nM | 5.15 |
| CHEMBL4791607 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4800037 | — | IC50 | = | 10980.0 | nM | 4.96 |
| CHEMBL4795593 | — | IC50 | = | 18090.0 | nM | 4.74 |
| CHEMBL4758137 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4748415 | — | IC50 | > | 50000.0 | nM | - |