Assay Detail
Functional
CHEMBL4708512
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Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
34
Total Activities
34
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 antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 4.79 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.11 |
| CHEMBL4789286 | — | — | 1 | 5.42 |
| CHEMBL4762165 | — | — | 1 | 5.38 |
| CHEMBL4787616 | — | — | 1 | 5.32 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 5.28 |
| CHEMBL4779676 | — | — | 1 | 5.09 |
| CHEMBL4800491 | — | — | 1 | 5.03 |
| CHEMBL4754104 | — | — | 1 | 4.93 |
| CHEMBL4797662 | — | — | 1 | 4.88 |
| CHEMBL4787376 | — | — | 1 | 4.86 |
| CHEMBL4783784 | — | — | 1 | 4.82 |
| CHEMBL4784010 | — | — | 1 | 4.75 |
| CHEMBL4751575 | — | — | 1 | 4.70 |
| CHEMBL4763694 | — | — | 1 | 4.69 |
| CHEMBL4750496 | — | — | 1 | 4.63 |
| CHEMBL4760454 | — | — | 1 | 4.63 |
| CHEMBL4799310 | — | — | 1 | 4.62 |
| CHEMBL4764011 | — | — | 1 | 4.60 |
| CHEMBL4749348 | — | — | 1 | 4.59 |
| CHEMBL4796277 | — | — | 1 | 4.58 |
| CHEMBL4743716 | — | — | 1 | 4.56 |
| CHEMBL4762510 | — | — | 1 | 4.55 |
| CHEMBL4786862 | — | — | 1 | 4.53 |
| CHEMBL4758340 | — | — | 1 | 4.52 |
| CHEMBL4745369 | — | — | 1 | 4.48 |
| CHEMBL4744140 | — | — | 1 | 4.44 |
| CHEMBL4743425 | — | — | 1 | 4.44 |
| CHEMBL4784801 | — | — | 1 | 4.43 |
| CHEMBL4761693 | — | — | 1 | 4.41 |
| CHEMBL4743435 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4789286 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL4762165 | — | IC50 | = | 4220.0 | nM | 5.38 |
| CHEMBL4787616 | — | IC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 5290.0 | nM | 5.28 |
| CHEMBL4779676 | — | IC50 | = | 8090.0 | nM | 5.09 |
| CHEMBL4800491 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4754104 | — | IC50 | = | 11750.0 | nM | 4.93 |
| CHEMBL4797662 | — | IC50 | = | 13090.0 | nM | 4.88 |
| CHEMBL4787376 | — | IC50 | = | 13860.0 | nM | 4.86 |
| CHEMBL4783784 | — | IC50 | = | 15090.0 | nM | 4.82 |
| CHEMBL4784010 | — | IC50 | = | 17620.0 | nM | 4.75 |
| CHEMBL4751575 | — | IC50 | = | 20090.0 | nM | 4.70 |
| CHEMBL4763694 | — | IC50 | = | 20390.0 | nM | 4.69 |
| CHEMBL4760454 | — | IC50 | = | 23390.0 | nM | 4.63 |
| CHEMBL4750496 | — | IC50 | = | 23380.0 | nM | 4.63 |
| CHEMBL4799310 | — | IC50 | = | 24120.0 | nM | 4.62 |
| CHEMBL4764011 | — | IC50 | = | 25180.0 | nM | 4.60 |
| CHEMBL4749348 | — | IC50 | = | 25790.0 | nM | 4.59 |
| CHEMBL4796277 | — | IC50 | = | 26210.0 | nM | 4.58 |
| CHEMBL4743716 | — | IC50 | = | 27810.0 | nM | 4.56 |
| CHEMBL4762510 | — | IC50 | = | 28280.0 | nM | 4.55 |
| CHEMBL4786862 | — | IC50 | = | 29230.0 | nM | 4.53 |
| CHEMBL4758340 | — | IC50 | = | 30340.0 | nM | 4.52 |
| CHEMBL4745369 | — | IC50 | = | 33310.0 | nM | 4.48 |
| CHEMBL4744140 | — | IC50 | = | 36230.0 | nM | 4.44 |
| CHEMBL4743425 | — | IC50 | = | 36230.0 | nM | 4.44 |
| CHEMBL4784801 | — | IC50 | = | 37170.0 | nM | 4.43 |
| CHEMBL4761693 | — | IC50 | = | 38910.0 | nM | 4.41 |
| CHEMBL4743435 | — | IC50 | = | 46140.0 | nM | 4.34 |
| CHEMBL4761509 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4763845 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4791684 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4748259 | — | IC50 | > | 50000.0 | nM | - |