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Compound Detail

CHEMBL3218481

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Cc1cnc(NC(=O)c2cc(Oc3ccc(C#N)cc3)c3cc(C)oc3c2)cn1

Basic Information

ChEMBL ID CHEMBL3218481
Phase Preclinical
Structure Type MOL
InChI Key VXTAHUFATFVDFI-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
4.76
ALogP
6
HBA
1
HBD
101.0
PSA (Ų)
0.54
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16N4O3
MW 384.40
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.04

Activity Summary

EC50 1 meas. best 5.51
IC50 1 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 5.51 5.51 3061.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.4 5.4 4000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 29.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00116G Hexokinase-4 1
- 10.1039/C1MD00116G Liver microsome 1
- 10.1039/C1MD00116G ADMET 1
- 10.1039/C1MD00116G No relevant target 1
- 10.1039/C1MD00116G Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine