Assay Detail
Binding
CHEMBL4387563
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Inhibition of 6x-His-tagged and SUMO tagged human PYCR1 expressed in Escherichia coli BL21 (DE3) cells assessed as reduction in NADH oxidation incubated for 1 hr
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Pyrroline-5-carboxylate reductase 1, mitochondrial (CHEMBL4296002) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A fragment-like approach to PYCR1 inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 61 | 4.14 | 5.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4442920 | — | — | 1 | 5.06 |
| CHEMBL4452615 | — | — | 1 | 5.04 |
| CHEMBL4462797 | — | — | 1 | 5.01 |
| CHEMBL4554584 | — | — | 1 | 4.89 |
| CHEMBL4440917 | — | — | 1 | 4.87 |
| CHEMBL4470037 | — | — | 1 | 4.80 |
| CHEMBL4578387 | — | — | 1 | 4.68 |
| CHEMBL4442170 | — | — | 1 | 4.68 |
| CHEMBL4538363 | — | — | 1 | 4.47 |
| CHEMBL4449993 | — | — | 1 | 4.42 |
| CHEMBL4471360 | — | — | 1 | 4.42 |
| CHEMBL4441578 | — | — | 1 | 4.40 |
| CHEMBL4441742 | — | — | 1 | 4.38 |
| CHEMBL4566601 | — | — | 1 | 4.37 |
| CHEMBL4545182 | — | — | 1 | 4.37 |
| CHEMBL4518799 | — | — | 1 | 4.28 |
| CHEMBL4521734 | — | — | 1 | 4.26 |
| CHEMBL4524807 | — | — | 1 | 4.24 |
| CHEMBL4471016 | — | — | 1 | 4.19 |
| CHEMBL4589637 | — | — | 1 | 4.18 |
| CHEMBL4531369 | — | — | 1 | 4.15 |
| CHEMBL4450640 | — | — | 1 | 4.04 |
| CHEMBL4582299 | — | — | 1 | 4.00 |
| CHEMBL4540573 | — | — | 1 | 4.00 |
| CHEMBL4572130 | — | — | 1 | 3.86 |
| CHEMBL4460666 | — | — | 1 | 3.85 |
| CHEMBL4551995 | — | — | 1 | 3.79 |
| CHEMBL4441214 | — | — | 1 | 3.73 |
| CHEMBL4582778 | — | — | 1 | 3.70 |
| CHEMBL673 | PARGYLINE | 4.0 | 1 | 3.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4442920 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4452615 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4462797 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4554584 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4440917 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL4470037 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4578387 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4442170 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4538363 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4449993 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4471360 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL4441578 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4441742 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL4545182 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL4566601 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL4518799 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL4521734 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL4524807 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL4471016 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL4589637 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL4531369 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL4450640 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL4582299 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL4540573 | — | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL4572130 | — | IC50 | = | 139000.0 | nM | 3.86 |
| CHEMBL4460666 | — | IC50 | = | 142000.0 | nM | 3.85 |
| CHEMBL4551995 | — | IC50 | = | 161000.0 | nM | 3.79 |
| CHEMBL4441214 | — | IC50 | = | 184000.0 | nM | 3.73 |
| CHEMBL4582778 | — | IC50 | = | 200000.0 | nM | 3.70 |
| CHEMBL673 | PARGYLINE | IC50 | = | 198000.0 | nM | 3.70 |
| CHEMBL4560325 | — | IC50 | = | 211000.0 | nM | 3.68 |
| CHEMBL4451218 | — | IC50 | = | 228000.0 | nM | 3.64 |
| CHEMBL4529176 | — | IC50 | = | 276000.0 | nM | 3.56 |
| CHEMBL4529927 | — | IC50 | = | 311000.0 | nM | 3.51 |
| CHEMBL4562371 | — | IC50 | = | 316000.0 | nM | 3.50 |
| CHEMBL4525457 | — | IC50 | = | 315000.0 | nM | 3.50 |
| CHEMBL4465015 | — | IC50 | = | 337000.0 | nM | 3.47 |
| CHEMBL4471459 | — | IC50 | = | 394000.0 | nM | 3.40 |
| CHEMBL4544449 | — | IC50 | = | 394000.0 | nM | 3.40 |
| CHEMBL4592190 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4545345 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4542486 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4529610 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4475507 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4539315 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL1182795 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4568453 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4547121 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4444403 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL4567902 | — | IC50 | > | 500000.0 | nM | - |