Assay Detail
Functional
CHEMBL4708513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A549 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 | A549 |
| 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 | 4.82 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.17 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 5.37 |
| CHEMBL4789286 | — | — | 1 | 5.36 |
| CHEMBL4787616 | — | — | 1 | 5.36 |
| CHEMBL4762165 | — | — | 1 | 5.28 |
| CHEMBL4779676 | — | — | 1 | 5.25 |
| CHEMBL4800491 | — | — | 1 | 5.07 |
| CHEMBL4797662 | — | — | 1 | 4.98 |
| CHEMBL4751575 | — | — | 1 | 4.95 |
| CHEMBL4754104 | — | — | 1 | 4.86 |
| CHEMBL4744140 | — | — | 1 | 4.83 |
| CHEMBL4783784 | — | — | 1 | 4.79 |
| CHEMBL4763694 | — | — | 1 | 4.78 |
| CHEMBL4762510 | — | — | 1 | 4.77 |
| CHEMBL4784010 | — | — | 1 | 4.74 |
| CHEMBL4799310 | — | — | 1 | 4.72 |
| CHEMBL4786862 | — | — | 1 | 4.71 |
| CHEMBL4743716 | — | — | 1 | 4.69 |
| CHEMBL4758340 | — | — | 1 | 4.67 |
| CHEMBL4796277 | — | — | 1 | 4.59 |
| CHEMBL4743425 | — | — | 1 | 4.59 |
| CHEMBL4787376 | — | — | 1 | 4.58 |
| CHEMBL4760454 | — | — | 1 | 4.58 |
| CHEMBL4749348 | — | — | 1 | 4.56 |
| CHEMBL4745369 | — | — | 1 | 4.53 |
| CHEMBL4743435 | — | — | 1 | 4.52 |
| CHEMBL4784801 | — | — | 1 | 4.50 |
| CHEMBL4761693 | — | — | 1 | 4.50 |
| CHEMBL4750496 | — | — | 1 | 4.43 |
| CHEMBL4764011 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL4789286 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL4787616 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL4762165 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL4779676 | — | IC50 | = | 5560.0 | nM | 5.25 |
| CHEMBL4800491 | — | IC50 | = | 8610.0 | nM | 5.07 |
| CHEMBL4797662 | — | IC50 | = | 10480.0 | nM | 4.98 |
| CHEMBL4751575 | — | IC50 | = | 11340.0 | nM | 4.95 |
| CHEMBL4754104 | — | IC50 | = | 13710.0 | nM | 4.86 |
| CHEMBL4744140 | — | IC50 | = | 14900.0 | nM | 4.83 |
| CHEMBL4783784 | — | IC50 | = | 16090.0 | nM | 4.79 |
| CHEMBL4763694 | — | IC50 | = | 16720.0 | nM | 4.78 |
| CHEMBL4762510 | — | IC50 | = | 16890.0 | nM | 4.77 |
| CHEMBL4784010 | — | IC50 | = | 18090.0 | nM | 4.74 |
| CHEMBL4799310 | — | IC50 | = | 19010.0 | nM | 4.72 |
| CHEMBL4786862 | — | IC50 | = | 19610.0 | nM | 4.71 |
| CHEMBL4743716 | — | IC50 | = | 20390.0 | nM | 4.69 |
| CHEMBL4758340 | — | IC50 | = | 21540.0 | nM | 4.67 |
| CHEMBL4796277 | — | IC50 | = | 25770.0 | nM | 4.59 |
| CHEMBL4743425 | — | IC50 | = | 25610.0 | nM | 4.59 |
| CHEMBL4787376 | — | IC50 | = | 26510.0 | nM | 4.58 |
| CHEMBL4760454 | — | IC50 | = | 26340.0 | nM | 4.58 |
| CHEMBL4749348 | — | IC50 | = | 27690.0 | nM | 4.56 |
| CHEMBL4745369 | — | IC50 | = | 29530.0 | nM | 4.53 |
| CHEMBL4743435 | — | IC50 | = | 29940.0 | nM | 4.52 |
| CHEMBL4784801 | — | IC50 | = | 31870.0 | nM | 4.50 |
| CHEMBL4761693 | — | IC50 | = | 31870.0 | nM | 4.50 |
| CHEMBL4750496 | — | IC50 | = | 37100.0 | nM | 4.43 |
| CHEMBL4764011 | — | IC50 | = | 37930.0 | nM | 4.42 |
| CHEMBL4761509 | — | IC50 | = | 40120.0 | nM | 4.40 |
| CHEMBL4763845 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4791684 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4748259 | — | IC50 | > | 50000.0 | nM | - |