PFI-3 10μM R03 exp144
Mechanism of Action
Inhibits SMARCA2/4 and PB1 bromodomain proteins, components of SNF/SWI chromatin remodelling complex
- Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor
Technical Notes
Compound References
- PubChem Name: (E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
- Synonyms: N/A
- CAS #: 1819363-80-8
- PubChem CID: 78243717
- IUPAC: (E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
- INCHI Name: InChI=1S/C19H19N3O2/c23-17-6-2-1-5-16(17)18(24)8-10-21-12-15-11-14(21)13-22(15)19-7-3-4-9-20-19/h1-10,14-15,23H,11-13H2/b10-8+/t14-,15-/m1/s1
- INCHI Key: INAICWLVUAKEPB-QSTFCLMHSA-N
- Molecular Weight: 321.4
- Canonical SMILES: C1C2CN(C1CN2C3=CC=CC=N3)C=CC(=O)C4=CC=CC=C4O
- Isomeric SMILES: C1[C@@H]2CN([C@H]1CN2C3=CC=CC=N3)/C=C/C(=O)C4=CC=CC=C4O
- Molecular Formula: C19H19N3O2
Compound Supplier
- Supplier Name: Structural Genomics Consortium
- Catalog #: N/A
- Lot #: N/A
Compound Characterization
- HRMS (ESI-TOF) m/z: [M+H]+ Calcd for C19H20N3O2 322.1550; found 322.1532
Dose Response Curve
- Platform ID: PFI3
- Min: -3.6038; Max: 30.9773
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | N/A |
| IC30 | N/A |
| IC40 | N/A |
| IC50 | N/A |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 03
- Dose: 10µM
- Days of incubation: 8
- Doublings: 7.6
- Numbers of reads: 8729480
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 |
|---|---|---|---|---|---|---|
| 0/0 | Scores |
PFI-3 10μM R03 exp144
PFI-3 10μM R03 exp144 vs VHL-ligand-1 20μM R07 exp421
Golgicide-A 2μM R03 exp121 vs PFI-3 10μM R03 exp144
