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Compound Detail

CHEMBL5999586

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CCn1c(-c2cccnc2[C@H](C)OC)c2c3cc(ccc31)-c1cc(O)cc(c1)C[C@H](NC(=O)[C@H](C(C)C)N(C)C(=O)C1CCN(C(=O)/C=C/CN(C)C)CC1)C(=O)N1CCC[C@H](N1)C(=O)OCC(C)(C)C2

Basic Information

ChEMBL ID CHEMBL5999586
Phase Preclinical
Structure Type MOL
InChI Key WJKFUACEGNTMHW-LOKQXVQNSA-N
2
Targets
15
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

975.2
MW (Da)
6.29
ALogP
12
HBA
3
HBD
178.9
PSA (Ų)
0.11
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C55H74N8O8
MW 975.24
Aromatic Rings 4
Heavy Atoms 71
NP-Likeness 0.10

Activity Summary

IC50 15 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GTPase KRas
CHEMBL2189121
IC50 6.26 5.5933 550.0 6
Unchecked
CHEMBL612545
IC50 6.26 6.0378 550.0 9

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
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... -
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... -
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... -
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