Assay Detail
Binding
CHEMBL4352157
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necroptosis measured after 24 hrs by cell titer-glo luminescent cell viability assay
72
Total Activities
72
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
Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 72 | 7.04 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4541955 | — | — | 1 | 8.70 |
| CHEMBL4514028 | — | — | 1 | 8.60 |
| CHEMBL4521353 | — | — | 1 | 8.40 |
| CHEMBL4514271 | — | — | 1 | 8.40 |
| CHEMBL4436215 | — | — | 1 | 8.40 |
| CHEMBL4537171 | — | — | 1 | 8.40 |
| CHEMBL4593226 | — | — | 1 | 8.19 |
| CHEMBL4446915 | — | — | 1 | 8.10 |
| CHEMBL4450890 | — | — | 1 | 8.10 |
| CHEMBL4584779 | — | — | 1 | 8.10 |
| CHEMBL4455042 | — | — | 1 | 8.00 |
| CHEMBL4548784 | — | — | 1 | 8.00 |
| CHEMBL4471642 | — | — | 1 | 7.89 |
| CHEMBL4576386 | — | — | 1 | 7.89 |
| CHEMBL4552893 | — | — | 1 | 7.80 |
| CHEMBL4454462 | — | — | 1 | 7.80 |
| CHEMBL4594130 | — | — | 1 | 7.60 |
| CHEMBL4561445 | — | — | 1 | 7.60 |
| CHEMBL4443534 | — | — | 1 | 7.50 |
| CHEMBL4556751 | — | — | 1 | 7.30 |
| CHEMBL4457026 | — | — | 1 | 7.20 |
| CHEMBL4545939 | — | — | 1 | 7.20 |
| CHEMBL4556131 | — | — | 1 | 7.20 |
| CHEMBL4565985 | — | — | 1 | 7.10 |
| CHEMBL4438495 | — | — | 1 | 7.10 |
| CHEMBL4588685 | — | — | 1 | 7.10 |
| CHEMBL4583157 | — | — | 1 | 7.00 |
| CHEMBL4540090 | — | — | 1 | 6.90 |
| CHEMBL4474320 | — | — | 1 | 6.90 |
| CHEMBL4454881 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4541955 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4514028 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4514271 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4436215 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4537171 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4521353 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4593226 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4446915 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4450890 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4584779 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4455042 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4548784 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4576386 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4471642 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4454462 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4552893 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4594130 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4561445 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4443534 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4556751 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4457026 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4545939 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4556131 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4588685 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4565985 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4438495 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4583157 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4540090 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4474320 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4454881 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4446523 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4465743 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4519627 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4545356 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4463322 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4436131 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4524420 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4575848 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4584741 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4526661 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4548719 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4544356 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL4437641 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1580000 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL4553214 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL4451628 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL4564157 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL4474301 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL4590117 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL4467752 | — | IC50 | = | 794.0 | nM | 6.10 |