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Compound Detail

CHEMBL3145419

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Cc1ccc2[nH]c(-n3[nH]c(C)c(Cc4ccccc4)c3=O)nc2c1

Basic Information

ChEMBL ID CHEMBL3145419
Phase Preclinical
Structure Type MOL
InChI Key IQOKQFQFGHZHJT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

318.4
MW (Da)
3.25
ALogP
3
HBA
2
HBD
66.5
PSA (Ų)
0.61
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18N4O
MW 318.38
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.12

Activity Summary

IC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-ketoglutarate-dependent dioxygenase alkB homolog 3
CHEMBL3112376
IC50 6.17 6.17 670.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 150.0 ng.hr.mL-1 Rattus norvegicus
AUC 690.0 ng.hr.mL-1 Rattus norvegicus
Cmax 1099.32 nM Rattus norvegicus
F 7.2 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24461353 10.1016/j.bmcl.2014.01.008 DU-145 5
24461353 10.1016/j.bmcl.2014.01.008 Rattus norvegicus 4
24461353 10.1016/j.bmcl.2014.01.008 Plasma 1
24461353 10.1016/j.bmcl.2014.01.008 Mus musculus 1
24461353 10.1016/j.bmcl.2014.01.008 Serum 1
24461353 10.1016/j.bmcl.2014.01.008 Alpha-ketoglutarate-dependent dioxygenase alkB homolog 3 1

Data from ChEMBL 36 via Core Engine