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Compound Detail

CHEMBL100979

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Cc1nc2ccccn2c1-c1ccnc(N)n1

Basic Information

ChEMBL ID CHEMBL100979
Phase Preclinical
Structure Type MOL
InChI Key LZURCICLQQQODJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

225.2
MW (Da)
1.68
ALogP
5
HBA
1
HBD
69.1
PSA (Ų)
0.68
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H11N5
MW 225.25
Aromatic Rings 3
Heavy Atoms 17
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.4 5.4 4000.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 5.1 5.1 8000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 21.38 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 50.12 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 4000.0 nM 5.4 Inhibition of Cyclin-dependent kinase 2 12941325
Cyclin-dependent kinase 4 IC50 = 8000.0 nM 5.1 Inhibition of Cyclin-dependent kinase 4 12941325

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 2
12941325 10.1016/s0960-894x(03)00638-3 Cyclin-dependent kinase 4 1
12941325 10.1016/s0960-894x(03)00638-3 Cyclin-dependent kinase 2 1
23374866 10.1016/j.bmcl.2013.01.012 Mitogen-activated protein kinase kinase kinase 14 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine