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Compound Detail

CHEMBL5863589

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C=CC(=O)N1CC[C@H](C(=O)N(C)[C@H](C(=O)N[C@H]2Cc3cc(O)cc(c3)-c3ccc4c(c3)c(c(-c3cccnc3[C@H](C)OC)n4CC)CC(C)(C)COC(=O)[C@@H]3CCCN(N3)C2=O)C(C)C)C1

Basic Information

ChEMBL ID CHEMBL5863589
Phase Preclinical
Structure Type MOL
InChI Key MTIZKJFMLDYTNE-YDDDOAIDSA-N
3
Targets
20
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

904.1
MW (Da)
5.97
ALogP
11
HBA
3
HBD
175.6
PSA (Ų)
0.13
QED
3
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C51H65N7O8
MW 904.12
Aromatic Rings 4
Heavy Atoms 66
NP-Likeness 0.08

Activity Summary

IC50 20 meas. best 7.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GTPase NRas
CHEMBL2079845
IC50 7.26 7.26 55.0 1
Unchecked
CHEMBL612545
IC50 7.26 5.7215 55.0 13
GTPase KRas
CHEMBL2189121
IC50 6.26 5.9267 550.0 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GTPase NRas IC50 = 55.0 nM 7.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 55.0 nM 7.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 550.0 nM 6.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
GTPase KRas IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -
Unchecked IC50 = 5500.0 nM 5.26 Biochemical Assay: A variety of Ras proteins may be inhibited by compounds of th... -

Data from ChEMBL 36 via Core Engine