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Compound Detail

CHEMBL4297584

TENALISIB
🧪 Phase II
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🧪 Phase II
CC[C@H](Nc1ncnc2[nH]cnc12)c1oc2ccccc2c(=O)c1-c1cccc(F)c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4297584
Name TENALISIB
Phase Phase II
Structure Type MOL
InChI Key HDXDQPRPFRKGKZ-INIZCTEOSA-N

Known Names

Rp-6530 RP6530 Tenalisib
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
3
Known Names
8
Indications
4
Mechanisms

Molecular Properties

415.4
MW (Da)
4.83
ALogP
6
HBA
2
HBD
96.7
PSA (Ų)
0.43
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -lisib

Extended Properties

Molecular Formula C23H18FN5O2
MW 415.43
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.68

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
PI3-kinase p110-delta subunit inhibitor INHIBITOR Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform ✓ ✓
PI3-kinase p110-gamma subunit inhibitor INHIBITOR Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform ✓ ✓
PI3-kinase p110-delta subunit inhibitor INHIBITOR Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform ✓ ✓
PI3-kinase p110-gamma subunit inhibitor INHIBITOR Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform ✓ ✓

Indications

Breast Neoplasms Leukemia, Lymphocytic, Chronic, B-Cell Lymphoma, Non-Hodgkin Lymphoma, T-Cell, Peripheral Hematologic Diseases Hodgkin Disease Lymphoma Lymphoma, T-Cell, Cutaneous

Activity Summary

IC50 6 meas. best 7.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
 IC50 7.61 7.6067 24.5 3
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
 IC50 7.48 7.48 33.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 24.5 nM 7.61 Inhibition of PI3Kdelta (unknown origin) 31581005
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 24.5 nM 7.61 Inhibition of P13Kdelta (unknown origin) 36462440
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 25.0 nM 7.6 Inhibition of PI3Kdelta (unknown origin) 30582813
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 33.0 nM 7.48 Inhibition of PI3Kgamma (unknown origin) 30582813
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 33.2 nM 7.48 Inhibition of PI3Kgamma (unknown origin) 31581005
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 33.2 nM 7.48 Inhibition of P13Kgamma (unknown origin) 36462440

Literature References

PubMed DOI Target Context # Activities
30582813 10.1021/acs.jmedchem.8b01298 Unchecked 2
30582813 10.1021/acs.jmedchem.8b01298 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
30582813 10.1021/acs.jmedchem.8b01298 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
31581005 10.1016/j.ejmech.2019.111718 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
31581005 10.1016/j.ejmech.2019.111718 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
36462440 10.1016/j.ejmech.2022.114971 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
36462440 10.1016/j.ejmech.2022.114971 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1

Data from ChEMBL 36 via Core Engine