TIC10 10μM R08 exp532
Mechanism of Action
Inhibits mitochondrial CLPP protease, a.k.a. ONC201, parent of ONC212, possible agonist of GPR132
- Class / Subclass 1: Proteostasis / Protease Inhibitor
- Class / Subclass 2: Signal Transduction / GPCR Agonist
Technical Notes
Compound References
- PubChem Name: 7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-A]pyrido[3,4-E]pyrimidin-5(4H)-one
- Synonyms: ONC-201
- CAS #: 1616632-77-9
- PubChem CID: 73777259
- IUPAC: 11-benzyl-7-[(2-methylphenyl)methyl]-2,5,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),5-dien-8-one
- INCHI Name: InChI=1S/C24H26N4O/c1-18-7-5-6-10-20(18)16-28-23(29)21-17-26(15-19-8-3-2-4-9-19)13-11-22(21)27-14-12-25-24(27)28/h2-10H,11-17H2,1H3
- INCHI Key: VLULRUCCHYVXOH-UHFFFAOYSA-N
- Molecular Weight: 386.5
- Canonical SMILES: CC1=CC=CC=C1CN2C(=O)C3=C(CCN(C3)CC4=CC=CC=C4)N5C2=NCC5
- Isomeric SMILES: N/A
- Molecular Formula: C24H26N4O
Compound Supplier
- Supplier Name: Med Chem Express
- Catalog #: HY-15615A
- Lot #: 14564
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C24H26N4O 387.21794; found 387.22085
Dose Response Curve
- Platform ID: TIC10
- Min: 0.7077; Max: 65.9742
| IC | Concentration (µM) |
|---|---|
| IC10 | 0.0216 |
| IC20 | 0.2196 |
| IC30 | 1.0240 |
| IC40 | 3.6190 |
| IC50 | 11.5200 |
| IC60 | 36.7000 |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 08
- Dose: 10µM
- Days of incubation: 8
- Doublings: 0.8
- Numbers of reads: 15670063
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 0/12 | Scores |