Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL5173264

INE-963
🧪 Phase II
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
🧪 Phase II
COc1nc(C(C)C)ccc1-c1cnc2sc(N3CCC(O)(CN)CC3)nn12

Basic Information

ChEMBL ID CHEMBL5173264
Name INE-963
Phase Phase II
Structure Type MOL
InChI Key JYHSRMKXBAPFST-UHFFFAOYSA-N

Known Names

Ine-963 Ine963
9
Targets
12
Activities
2
Assay Types
30
PK Parameters
17
Publications
2
Known Names
1
Indications

Molecular Properties

402.5
MW (Da)
2.27
ALogP
9
HBA
2
HBD
101.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Extended Properties

Molecular Formula C19H26N6O2S
MW 402.52
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.06

Indications

Malaria, Falciparum

Activity Summary

IC50 7 meas. best 5.44
EC50 5 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 9.4 8.665 0.4 4
Plasmodium vivax
CHEMBL613013
EC50 8.7 8.7 2.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.44 5.44 3600.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.35 5.35 4500.0 1
Cytochrome P450 2C19
CHEMBL3622
IC50 5.27 5.27 5400.0 1
Serine/threonine-protein kinase haspin
CHEMBL1075163
IC50 5.26 5.26 5500.0 1
Cytochrome P450 2B6
CHEMBL4729
IC50 5.22 5.22 6000.0 1
Cytochrome P450 2C8
CHEMBL3721
IC50 5.07 5.07 8500.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.64 4.64 23000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 8690.41 ng.hr.mL-1 Rattus norvegicus
AUC 5100.0 ng.hr.mL-1 Mus musculus
AUC 770.0 ng.hr.mL-1 Mus musculus
AUC 2300.0 ng.hr.mL-1 Mus musculus
AUC 680.0 ng.hr.mL-1 Mus musculus
AUC 1800.0 ng.hr.mL-1 Mus musculus
AUC 1300.0 ng.hr.mL-1 Mus musculus
AUC 3500.0 ng.hr.mL-1 Mus musculus
AUC 6900.0 ng.hr.mL-1 Mus musculus
AUC 16700.0 ng.hr.mL-1 Mus musculus
AUC 1700.0 ng.hr.mL-1 Mus musculus
AUC 4500.0 ng.hr.mL-1 Mus musculus
AUC 8200.0 ng.hr.mL-1 Mus musculus
AUC 29800.0 ng.hr.mL-1 Mus musculus
CL 25.4 mL.min-1.g-1 Homo sapiens
CL 29.0 mL.min-1.g-1 Rattus norvegicus
CL 25.0 mL.min-1.g-1 Mus musculus
CL 4.0 mL.min-1.g-1 Canis lupus familiaris
CL 25.0 mL.min-1.g-1 Canis lupus familiaris
CL 4.0 mL.min-1.kg-1 Mus musculus
CL 5.9 mL.min-1.kg-1 Rattus norvegicus
CL 5.4 mL.min-1.kg-1 Canis lupus familiaris
Cmax 397.5 nM Mus musculus
Cmax 198.75 nM Mus musculus
Cmax 3726.52 nM Mus musculus
Cmax 996.0 nM Rattus norvegicus
Cmax 1465.77 nM Mus musculus
Cmax 397.5 nM Mus musculus
Cmax 993.74 nM Mus musculus
Cmax 1490.61 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35229610 10.1021/acs.jmedchem.1c01995 ADMET 70
35229610 10.1021/acs.jmedchem.1c01995 Plasmodium falciparum 23
35229610 10.1021/acs.jmedchem.1c01995 No relevant target 5
35229610 10.1021/acs.jmedchem.1c01995 Unchecked 1
35229610 10.1021/acs.jmedchem.1c01995 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
35229610 10.1021/acs.jmedchem.1c01995 Cytochrome P450 2B6 1
35229610 10.1021/acs.jmedchem.1c01995 Cytochrome P450 2C8 1
35229610 10.1021/acs.jmedchem.1c01995 Cytochrome P450 2C19 1
35229610 10.1021/acs.jmedchem.1c01995 Cytochrome P450 2C9 1
35229610 10.1021/acs.jmedchem.1c01995 Plasmodium vivax 1
35229610 10.1021/acs.jmedchem.1c01995 MT4 1
35229610 10.1021/acs.jmedchem.1c01995 K562 1
35229610 10.1021/acs.jmedchem.1c01995 Serine/threonine-protein kinase pim-1 1
35229610 10.1021/acs.jmedchem.1c01995 Receptor-type tyrosine-protein kinase FLT3 1
35229610 10.1021/acs.jmedchem.1c01995 Voltage-gated inwardly rectifying potassium channel KCNH2 1
35229610 10.1021/acs.jmedchem.1c01995 HepG2 1
35229610 10.1021/acs.jmedchem.1c01995 Serine/threonine-protein kinase haspin 1

Data from ChEMBL 36 via Core Engine