Assay Detail
Binding
CHEMBL957604
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Inhibition of human PLD1 in Calu1 cells
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Calu-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.88 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2304616 | — | — | 1 | 8.70 |
| CHEMBL493521 | — | — | 1 | 8.70 |
| CHEMBL492561 | — | — | 1 | 8.52 |
| CHEMBL492558 | — | — | 1 | 8.52 |
| CHEMBL492559 | — | — | 1 | 8.46 |
| CHEMBL524182 | — | — | 1 | 8.43 |
| CHEMBL493010 | — | — | 1 | 8.40 |
| CHEMBL521990 | — | — | 1 | 8.40 |
| CHEMBL492972 | — | — | 1 | 8.40 |
| CHEMBL523011 | — | — | 1 | 8.40 |
| CHEMBL492704 | — | — | 1 | 8.26 |
| CHEMBL494145 | — | — | 1 | 8.19 |
| CHEMBL492971 | — | — | 1 | 8.15 |
| CHEMBL522488 | — | — | 1 | 8.13 |
| CHEMBL521677 | — | — | 1 | 8.10 |
| CHEMBL246032 | — | — | 1 | 8.10 |
| CHEMBL492589 | — | — | 1 | 8.00 |
| CHEMBL494183 | — | — | 1 | 8.00 |
| CHEMBL492588 | — | — | 1 | 7.96 |
| CHEMBL493736 | — | — | 1 | 7.92 |
| CHEMBL492369 | — | — | 1 | 7.92 |
| CHEMBL523162 | — | — | 1 | 7.75 |
| CHEMBL492797 | — | — | 1 | 7.68 |
| CHEMBL245621 | HALOPEMIDE | 2.0 | 1 | 7.68 |
| CHEMBL524008 | — | — | 1 | 7.46 |
| CHEMBL492379 | — | — | 1 | 7.42 |
| CHEMBL494007 | — | — | 1 | 7.40 |
| CHEMBL495349 | — | — | 1 | 7.37 |
| CHEMBL492572 | — | — | 1 | 7.34 |
| CHEMBL492380 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2304616 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL493521 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL492561 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL492558 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL492559 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL524182 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL493010 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL521990 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL492972 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL523011 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL492704 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL494145 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL492971 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL522488 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL246032 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL521677 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL494183 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL492589 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL492588 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL493736 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL492369 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL523162 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL492797 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL245621 | HALOPEMIDE | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL524008 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL492379 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL494007 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL495349 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL492572 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL492380 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL494008 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL494587 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL494842 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL495018 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL523496 | — | IC50 | = | 130.0 | nM | 6.89 |