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Compound Detail

CHEMBL3736210

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Cc1nc2cnc(Nc3ccnc(OCC(C)(C)S(C)(=O)=O)n3)cc2n1C(C)C

Basic Information

ChEMBL ID CHEMBL3736210
Phase Preclinical
Structure Type MOL
InChI Key SHYWETJFHVMCJS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
3.06
ALogP
9
HBA
1
HBD
111.9
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H26N6O3S
MW 418.52
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.22

Activity Summary

Ki 2 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 7.28 6.48 52.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 53.0 mL.min-1.kg-1 Rattus norvegicus
CL 156.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26455919 10.1021/acs.jmedchem.5b01412 Epidermal growth factor receptor 2
26455919 10.1021/acs.jmedchem.5b01412 Rattus norvegicus 2
26455919 10.1021/acs.jmedchem.5b01412 No relevant target 1
26455919 10.1021/acs.jmedchem.5b01412 Liver microsome 1
26455919 10.1021/acs.jmedchem.5b01412 Hepatocyte 1

Data from ChEMBL 36 via Core Engine