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Compound Detail

CHEMBL5744081

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C=CC(=O)Nc1ccc(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)cn1

Basic Information

ChEMBL ID CHEMBL5744081
Phase Preclinical
Structure Type MOL
InChI Key XYGUJQWVASQIJN-LRPVSRHNSA-N
2
Targets
21
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

927.1
MW (Da)
6.77
ALogP
12
HBA
4
HBD
197.3
PSA (Ų)
0.08
QED
3
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H62N8O8
MW 927.12
Aromatic Rings 5
Heavy Atoms 68

Activity Summary

IC50 21 meas. best 7.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GTPase KRas
CHEMBL2189121
IC50 7.26 5.885 55.0 8
Unchecked
CHEMBL612545
IC50 7.26 6.4138 55.0 13

Activity Data Samples

Top measurements by pChEMBL value

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

Data from ChEMBL 36 via Core Engine