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Compound Detail

CHEMBL1269516

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CC1(C)[C@@H](O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)OCc6ccccc6)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12

Basic Information

ChEMBL ID CHEMBL1269516
Phase Preclinical
Structure Type MOL
InChI Key UNRVOFRDIGTQBY-CJBAOGIUSA-N
14
Targets
17
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

560.8
MW (Da)
8.07
ALogP
4
HBA
1
HBD
63.6
PSA (Ų)
0.38
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H52O4
MW 560.82
Aromatic Rings 1
Heavy Atoms 41
NP-Likeness 2.46

Activity Summary

IC50 17 meas. best 5.56

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SW-1736
CHEMBL614773
IC50 5.56 5.56 2740.0 1
FaDu
CHEMBL612250
IC50 5.26 5.26 5480.0 1
A549
CHEMBL392
IC50 5.21 5.21 6150.0 1
SW480
CHEMBL612544
IC50 5.21 5.21 6170.0 1
8505C
CHEMBL1075387
IC50 5.09 5.09 8100.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.97 4.8833 10670.0 3
HT-29
CHEMBL384
IC50 4.94 4.94 11480.0 1
MCF7
CHEMBL387
IC50 4.87 4.87 13490.0 1
HCT-116
CHEMBL394
IC50 4.69 4.69 20570.0 1
A2780
CHEMBL614004
IC50 4.69 4.69 20320.0 1
ADMET
CHEMBL612558
IC50 4.68 4.68 21020.0 1
DLD-1
CHEMBL614285
IC50 4.64 4.64 22690.0 1
A-431
CHEMBL614069
IC50 4.63 4.63 23580.0 1
HCT-8
CHEMBL613510
IC50 4.6 4.6 25230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
SW-1736 IC50 = 2740.0 nM 5.56 Cytotoxicity against human SW1736 cells after 96 hrs by SRB assay 20932766
FaDu IC50 = 5480.0 nM 5.26 Cytotoxicity against human FADU cells after 96 hrs by SRB assay 20932766
A549 IC50 = 6150.0 nM 5.21 Cytotoxicity against human A549 cells after 96 hrs by SRB assay 20932766
SW480 IC50 = 6170.0 nM 5.21 Cytotoxicity against human SW480 cells after 96 hrs by SRB assay 20932766
8505C IC50 = 8100.0 nM 5.09 Cytotoxicity against human 8505C cells after 96 hrs by SRB assay 20932766
NON-PROTEIN TARGET IC50 = 10670.0 nM 4.97 Cytotoxicity against human A253 cells after 96 hrs by SRB assay 20932766
HT-29 IC50 = 11480.0 nM 4.94 Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay 20932766
NON-PROTEIN TARGET IC50 = 11540.0 nM 4.94 Cytotoxicity against human Lipo cells after 96 hrs by SRB assay 20932766
MCF7 IC50 = 13490.0 nM 4.87 Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay 20932766
NON-PROTEIN TARGET IC50 = 18190.0 nM 4.74 Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay 20932766
A2780 IC50 = 20320.0 nM 4.69 Cytotoxicity against human A2780 cells after 96 hrs by SRB assay 20932766
HCT-116 IC50 = 20570.0 nM 4.69 Cytotoxicity against human HCT116 cells after 96 hrs by SRB assay 20932766
ADMET IC50 = 21020.0 nM 4.68 Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay 20932766
DLD-1 IC50 = 22690.0 nM 4.64 Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay 20932766
A-431 IC50 = 23580.0 nM 4.63 Cytotoxicity against human A431 cells after 96 hrs by SRB assay 20932766
HCT-8 IC50 = 25230.0 nM 4.6 Cytotoxicity against human HCT8 cells after 96 hrs by SRB assay 20932766

Literature References

Data from ChEMBL 36 via Core Engine