GtoPdb Ligand ID: 10163

Synonyms: RV-6153
Compound class: Synthetic organic
Comment: RV6153 is a clinical stage PI3Kγδ inhibitor [1] that is being developed by Janssen Biotech subsidiary RespiVert. The chemical structure is claimed in patent US9227977B2 [2]. It is a derivative of RV1729. RV6153 is selective for PI3Kγδ over the α and β enzyme isoforms.
2D Structure
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Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 2
Rotatable bonds 13
Topological polar surface area 152.43
Molecular weight 717.23
XLogP 5.88
No. Lipinski's rules broken 2
Canonical SMILES COCCOCCOCC#Cc1cccc2c1c(=O)n(c(n2)Cn1nc(c2c1ncnc2N)c1cc(O)cc(c1)F)Cc1ccccc1C(F)(F)F
Isomeric SMILES COCCOCCOCC#Cc1cccc2c1c(=O)n(c(n2)Cn1nc(c2c1ncnc2N)c1cc(O)cc(c1)F)Cc1ccccc1C(F)(F)F
InChI InChI=1S/C36H31F4N7O5/c1-50-12-13-52-15-14-51-11-5-8-22-7-4-10-28-30(22)35(49)46(19-23-6-2-3-9-27(23)36(38,39)40)29(44-28)20-47-34-31(33(41)42-21-43-34)32(45-47)24-16-25(37)18-26(48)17-24/h2-4,6-7,9-10,16-18,21,48H,11-15,19-20H2,1H3,(H2,41,42,43)
No information available.
Summary of Clinical Use
A Phase 1 study of RV6153 in healthy volunteers and asthma patients (NCT02517359) was terminated as the preset pharmacokinetic stopping criteria were met at lower doses than expected.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02517359 A Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Repeat Doses of RV6153 Phase 1 Interventional Respivert Ltd