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Compound Detail

CHEMBL2409196

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CC(=O)Nc1cc(Nc2cc(NC3COC3)n3ncc(C#N)c3n2)c(F)cc1C

Basic Information

ChEMBL ID CHEMBL2409196
Phase Preclinical
Structure Type MOL
InChI Key KZBVYCAEPIFCJY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

395.4
MW (Da)
2.56
ALogP
8
HBA
3
HBD
116.4
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18FN7O2
MW 395.40
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.91

Activity Summary

IC50 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.68 7.68 21.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 6.0 mL.min-1.g-1 Rattus norvegicus
Fu 0.26 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 21.0 nM 7.68 Inhibition of casein kinase-2 in human HCT116 cells assessed as inhibition of AK... 24900749

Literature References

PubMed DOI Target Context # Activities
24900749 10.1021/ml400197u No relevant target 2
24900749 10.1021/ml400197u HCT-116 1
24900749 10.1021/ml400197u Unchecked 1
24900749 10.1021/ml400197u Casein kinase II subunit alpha 1
24900749 10.1021/ml400197u Liver microsomes 1
24900749 10.1021/ml400197u Voltage-gated inwardly rectifying potassium channel KCNH2 1
24900749 10.1021/ml400197u Plasma 1

Data from ChEMBL 36 via Core Engine