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Compound Detail

CHEMBL3355538

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CN1Cc2cc(Nc3ncc4c(=O)n(-c5c(Cl)cccc5Cl)c5nccn5c4n3)ccc2C(C)(C)C1

Basic Information

ChEMBL ID CHEMBL3355538
Phase Preclinical
Structure Type MOL
InChI Key FIEFUTLSNLZAGA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

520.4
MW (Da)
5.20
ALogP
8
HBA
1
HBD
80.3
PSA (Ų)
0.35
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23Cl2N7O
MW 520.42
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -0.91

Activity Summary

EC50 1 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H1299
CHEMBL612255
EC50 6.64 6.64 230.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5100.12 ng.hr.mL-1 Mus musculus
CL 16.17 mL.min-1.kg-1 Mus musculus
F 49.0 % Mus musculus
T1/2 3.9 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NCI-H1299 EC50 = 230.0 nM 6.64 Cytotoxicity against human NCI-H1299 cells assessed as cell viability after 72 h... 25589931

Literature References

PubMed DOI Target Context # Activities
25589931 10.1021/ml5002745 Mus musculus 4
25589931 10.1021/ml5002745 Wee1-like protein kinase 2
25589931 10.1021/ml5002745 NCI-H1299 1

Data from ChEMBL 36 via Core Engine