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Compound Detail

CHEMBL282939

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COc1cc([C@@H]2c3[nH]c4ccccc4c3C[C@H]3C(=O)NCC(=O)N23)cc(OC)c1O

Basic Information

ChEMBL ID CHEMBL282939
Phase Preclinical
Structure Type MOL
InChI Key HTPGHTCBAMDAAS-MGPUTAFESA-N
9
Targets
9
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

407.4
MW (Da)
1.86
ALogP
5
HBA
3
HBD
103.9
PSA (Ų)
0.61
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N3O5
MW 407.43
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness 0.26

Activity Summary

IC50 9 meas. best 4.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Panel leukemia (Carcinoma cell lines)
CHEMBL614083
IC50 4.42 4.42 38018.9 1
CNS cell
CHEMBL614782
IC50 4.42 4.42 38018.9 1
Melanoma cell
CHEMBL614126
IC50 4.34 4.34 45708.8 1
Colon cell
CHEMBL614469
IC50 4.33 4.33 46773.5 1
Breast carcinoma cell
CHEMBL614026
IC50 4.31 4.31 48977.9 1
Renal cell
CHEMBL614738
IC50 4.26 4.26 54954.1 1
NSO
CHEMBL615003
IC50 4.25 4.25 56234.1 1
Ovarian carcinoma cell
CHEMBL614667
IC50 4.18 4.18 66069.3 1
Prostate cell
CHEMBL614850
IC50 4.15 4.15 70794.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10780915 10.1021/jm9905662 3Y1 cell line 3
11392530 10.1016/s0960-894x(01)00136-6 NCI-H520 3
11392530 10.1016/s0960-894x(01)00136-6 PC-3 3
10780915 10.1021/jm9905662 Panel leukemia (Carcinoma cell lines) 1
10780915 10.1021/jm9905662 NSO 1
10780915 10.1021/jm9905662 Colon cell 1
10780915 10.1021/jm9905662 CNS cell 1
10780915 10.1021/jm9905662 Melanoma cell 1
10780915 10.1021/jm9905662 Ovarian carcinoma cell 1
10780915 10.1021/jm9905662 Renal cell 1
10780915 10.1021/jm9905662 Prostate cell 1
10780915 10.1021/jm9905662 Breast carcinoma cell 1
11392530 10.1016/s0960-894x(01)00136-6 DNA topoisomerase II 1

Data from ChEMBL 36 via Core Engine