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Compound Detail

CHEMBL510311

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CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C(F)F)c4ccccc4)C[C@@](O)([C@@H](OC(=O)c4cccc(F)c4)[C@H]21)C3(C)C

Basic Information

ChEMBL ID CHEMBL510311
Phase Preclinical
Structure Type MOL
InChI Key JTZHFBHKINHSON-AYORVWLJSA-N
2
Targets
6
Activities
1
Assay Types
8
PK Parameters
7
Publications
0
Known Names

Molecular Properties

861.9
MW (Da)
3.64
ALogP
14
HBA
5
HBD
224.4
PSA (Ų)
0.13
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H50F3NO14
MW 861.86
Aromatic Rings 2
Heavy Atoms 61
NP-Likeness 1.64

Activity Summary

IC50 6 meas. best 10.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SK-OV-3
CHEMBL614925
IC50 10.3 10.3 0.1 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 9.79 9.53 0.2 5

Pharmacokinetic Data

Parameter Value Units Species
AUC 1932.0 ng.hr.mL-1 Rattus norvegicus
AUC 1989.0 ng.hr.mL-1 Rattus norvegicus
CL 42.5 mL.min-1.kg-1 Rattus norvegicus
CL 4.67 mL.min-1.kg-1 Homo sapiens
MRT 2.4 hr Rattus norvegicus
T1/2 4.443 hr Homo sapiens
T1/2 10.15 hr Rattus norvegicus
Vd 36.2 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine