Assay Detail
Binding
CHEMBL4352155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2''3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido-[1,2-a]indol-5-ium-2-sulfonate binding to human GST/His-tagged RIP1 (1 to 375) expressed in baculovirus expression system preincubated for 10 mins followed by fluorescently labeled ATP-competitive ligand addition and measured after 20 mins by fluorescence polarization 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 | 7.84 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474301 | — | — | 1 | 8.00 |
| CHEMBL4594130 | — | — | 1 | 8.00 |
| CHEMBL4454462 | — | — | 1 | 8.00 |
| CHEMBL4457026 | — | — | 1 | 8.00 |
| CHEMBL4443534 | — | — | 1 | 8.00 |
| CHEMBL4556751 | — | — | 1 | 8.00 |
| CHEMBL4454881 | — | — | 1 | 8.00 |
| CHEMBL4561445 | — | — | 1 | 8.00 |
| CHEMBL4450890 | — | — | 1 | 8.00 |
| CHEMBL4541955 | — | — | 1 | 8.00 |
| CHEMBL4514271 | — | — | 1 | 8.00 |
| CHEMBL4545939 | — | — | 1 | 8.00 |
| CHEMBL4455042 | — | — | 1 | 8.00 |
| CHEMBL4471642 | — | — | 1 | 8.00 |
| CHEMBL4436131 | — | — | 1 | 8.00 |
| CHEMBL4527680 | — | — | 1 | 8.00 |
| CHEMBL4474937 | — | — | 1 | 8.00 |
| CHEMBL4564157 | — | — | 1 | 8.00 |
| CHEMBL4452678 | — | — | 1 | 8.00 |
| CHEMBL4554458 | — | — | 1 | 8.00 |
| CHEMBL4519892 | — | — | 1 | 8.00 |
| CHEMBL4575848 | — | — | 1 | 8.00 |
| CHEMBL4565985 | — | — | 1 | 8.00 |
| CHEMBL4553214 | — | — | 1 | 8.00 |
| CHEMBL4474320 | — | — | 1 | 8.00 |
| CHEMBL4463322 | — | — | 1 | 8.00 |
| CHEMBL4526661 | — | — | 1 | 8.00 |
| CHEMBL4448942 | — | — | 1 | 8.00 |
| CHEMBL4588685 | — | — | 1 | 8.00 |
| CHEMBL4548719 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514028 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4443534 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4457026 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4454462 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4594130 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4552893 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4465743 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4524420 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4583157 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4548784 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4584779 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4437098 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4537171 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4556751 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4593226 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4436215 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4576386 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4556131 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4533161 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4436896 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4544356 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4446523 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4446758 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4448908 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4451628 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4564157 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4548719 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4588685 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4448942 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4526661 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4463322 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4474320 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4553214 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4565985 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4575848 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4519892 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4554458 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4452678 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4527680 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4474937 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4474301 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4436131 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4471642 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4455042 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4545939 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4514271 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4541955 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4450890 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4561445 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4454881 | — | IC50 | = | 10.0 | nM | 8.00 |