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Compound Detail

CHEMBL4636230

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COc1cc(C(=O)N2CCOCC2)ccc1Nc1nc2ccc(-c3ccc(NC(=O)Cc4ccc(F)cc4)cc3)cn2n1

Basic Information

ChEMBL ID CHEMBL4636230
Phase Preclinical
Structure Type MOL
InChI Key VCZWYYTXLPJTGN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

580.6
MW (Da)
4.94
ALogP
8
HBA
2
HBD
110.1
PSA (Ų)
0.27
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H29FN6O4
MW 580.62
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.84

Activity Summary

IC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HeLa
CHEMBL399
IC50 6.85 6.85 140.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 20.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HeLa IC50 = 140.0 nM 6.85 Antiproliferative activity against human HeLa cells after 96 hrs by crystal viol... 32338514

Literature References

PubMed DOI Target Context # Activities
32338514 10.1021/acs.jmedchem.9b02035 ADMET 4
32338514 10.1021/acs.jmedchem.9b02035 Dual specificity protein kinase TTK 1
32338514 10.1021/acs.jmedchem.9b02035 HeLa 1

Data from ChEMBL 36 via Core Engine