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Compound Detail

CHEMBL267891

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C1CCC(NC2CCCCC2)CC1.CC[C@@H](c1ccc(O)cc1)[C@H](CCCCn1cc(C(=O)O)cn1)c1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL267891
Phase Preclinical
Structure Type MOL
InChI Key DRDJJPJADUKQIZ-PEADMDKFSA-N
Parent Compound CHEMBL1182813
Active Moiety CHEMBL1182813
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
5.14
ALogP
5
HBA
3
HBD
95.6
PSA (Ų)
0.40
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H51N3O4
MW 589.82
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.43

Activity Summary

EC50 1 meas. best 5.8
IC50 1 meas. best 4.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ishikawa
CHEMBL614649
EC50 5.8 5.8 1600.0 1
Estrogen receptor
CHEMBL2094114
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Ishikawa EC50 = 1600.0 nM 5.8 Agonist activity in Ishikawa human endometrial cells -
Estrogen receptor IC50 = 12000.0 nM 4.92 Binding affinity for rat estrogen receptor -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00165-5 Estrogen receptor 2
- 10.1016/0960-894X(96)00165-5 Ishikawa 1

Data from ChEMBL 36 via Core Engine