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Compound Detail

CHEMBL4845680

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C[C@@H]1Cc2c([nH]c3ccccc23)[C@@H](c2c(F)cc(O[C@H]3CCN(CCCF)C3)cc2F)N1CC(F)(F)CO

Basic Information

ChEMBL ID CHEMBL4845680
Phase Preclinical
Structure Type MOL
InChI Key MYPDGDGBPYLRFG-DLEQGYHRSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

537.6
MW (Da)
5.22
ALogP
4
HBA
2
HBD
51.7
PSA (Ų)
0.37
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32F5N3O2
MW 537.57
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.33

Activity Summary

EC50 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
EC50 9.52 9.52 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 15.0 mL.min-1.kg-1 Homo sapiens
CL 35.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 EC50 = 0.3 nM 9.52 Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cel... 34251202

Literature References

PubMed DOI Target Context # Activities
34251202 10.1021/acs.jmedchem.1c00847 Estrogen receptor 3
34251202 10.1021/acs.jmedchem.1c00847 ADMET 2
34251202 10.1021/acs.jmedchem.1c00847 MCF7 1
34251202 10.1021/acs.jmedchem.1c00847 No relevant target 1

Data from ChEMBL 36 via Core Engine