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Compound Detail

CHEMBL4786559

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COC[C@H](C)N[C@H]1CC[C@H](Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1

Basic Information

ChEMBL ID CHEMBL4786559
Phase Preclinical
Structure Type MOL
InChI Key XWQVQSXLXAXOPJ-ACRUOGEOSA-N
14
Targets
14
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

513.1
MW (Da)
4.88
ALogP
8
HBA
3
HBD
104.1
PSA (Ų)
0.41
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H37ClN6O2
MW 513.09
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -0.98

Activity Summary

IC50 14 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
OCI-Ly10
CHEMBL4483285
IC50 8.68 8.68 2.1 1
CCRF-CEM
CHEMBL382
IC50 8.48 8.48 3.3 1
Z-138
CHEMBL4483276
IC50 8.43 8.43 3.7 1
CDK9/cyclin T1
CHEMBL2111389
IC50 8.3 8.3 5.0 1
Unchecked
CHEMBL612545
IC50 8.28 8.28 5.2 1
MV4-11
CHEMBL613835
IC50 8.27 8.27 5.4 1
HL-60
CHEMBL383
IC50 8.24 8.24 5.7 1
MM1.S
CHEMBL4296471
IC50 8.2 8.2 6.3 1
Kasumi 1
CHEMBL613988
IC50 8.17 8.17 6.8 1
MOLT-4
CHEMBL614177
IC50 8.05 8.05 9.0 1
JeKo-1
CHEMBL4296445
IC50 8.0 8.0 10.0 1
Raji
CHEMBL614628
IC50 7.96 7.96 11.0 1
RPMI-8226
CHEMBL614882
IC50 7.85 7.85 14.0 1
TMD8
CHEMBL4296503
IC50 7.82 7.82 15.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
OCI-Ly10 IC50 = 2.1 nM 8.68 Antiproliferative activity against human OCILY10 cells assessed as reduction in ... 34477384
CCRF-CEM IC50 = 3.3 nM 8.48 Antiproliferative activity against human CCRF-CEM cells assessed as reduction in... 34477384
Z-138 IC50 = 3.7 nM 8.43 Antiproliferative activity against human Z138 cells assessed as reduction in cel... 34477384
CDK9/cyclin T1 IC50 = 4.96 nM 8.3 Inhibition of CDK9/cyclin T1 (unknown origin) incubated for 2 hrs in presence of... 34477384
Unchecked IC50 = 5.2 nM 8.28 Antiproliferative activity against human MINO cells assessed as reduction in cel... 34477384
MV4-11 IC50 = 5.4 nM 8.27 Antiproliferative activity against human MV4-11 cells assessed as reduction in c... 34477384
HL-60 IC50 = 5.7 nM 8.24 Antiproliferative activity against human HL-60 cells assessed as reduction in ce... 34477384
MM1.S IC50 = 6.3 nM 8.2 Antiproliferative activity against human MM1.S cells assessed as reduction in ce... 34477384
Kasumi 1 IC50 = 6.8 nM 8.17 Antiproliferative activity against human Kasumi 1 cells assessed as reduction in... 34477384
MOLT-4 IC50 = 9.0 nM 8.05 Antiproliferative activity against human MOLT4 cells incubated for 72 hrs by cel... 32866383
JeKo-1 IC50 = 10.0 nM 8.0 Antiproliferative activity against human JeKo-1 cells assessed as reduction in c... 34477384
Raji IC50 = 11.0 nM 7.96 Antiproliferative activity against human Raji cells assessed as reduction in cel... 34477384
RPMI-8226 IC50 = 14.0 nM 7.85 Antiproliferative activity against human RPMI-8226 cells assessed as reduction i... 34477384
TMD8 IC50 = 15.0 nM 7.82 Antiproliferative activity against human TMD8 cells assessed as reduction in cel... 34477384

Literature References

Data from ChEMBL 36 via Core Engine