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Compound Detail

CHEMBL4849535

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C[C@H](C(=O)N[C@H](CO)c1cc(F)cc(OCCN(C)C)c1)N1Cc2ccc(-c3nc(NC4CCOCC4)ncc3Cl)cc2C1=O

Basic Information

ChEMBL ID CHEMBL4849535
Phase Preclinical
Structure Type MOL
InChI Key WAYUBBBDNAECIV-WHLCRQNOSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

641.1
MW (Da)
3.66
ALogP
9
HBA
3
HBD
129.2
PSA (Ų)
0.27
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38ClFN6O5
MW 641.14
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -1.05

Activity Summary

IC50 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A-375
CHEMBL613859
IC50 6.92 6.92 120.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Homo sapiens
T1/2 0.1667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A-375 IC50 = 120.0 nM 6.92 Antiproliferative activity against human A-375 cells assessed as reduction in ce... 34387469

Literature References

PubMed DOI Target Context # Activities
34387469 10.1021/acs.jmedchem.1c00905 A-375 1
34387469 10.1021/acs.jmedchem.1c00905 ADMET 1
34387469 10.1021/acs.jmedchem.1c00905 Cytochrome P450 3A4 1
34387469 10.1021/acs.jmedchem.1c00905 Mitogen-activated protein kinase 1 1

Data from ChEMBL 36 via Core Engine