Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL3656841

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
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 CHEMBL3656841
Phase Preclinical
Structure Type MOL
InChI Key XWQVQSXLXAXOPJ-NJDAHSKKSA-N
19
Targets
22
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 Small molecule
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 22 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/Cyclin K
CHEMBL3038475
IC50 8.7 8.7 2.0 1
MV4-11
CHEMBL613835
IC50 8.52 8.52 3.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 8.45 8.42 3.6 2
CDK9/cyclin T1
CHEMBL2111389
IC50 8.43 8.43 3.8 1
CESS
CHEMBL2366361
IC50 8.0 8.0 10.0 1
HT-29
CHEMBL384
IC50 7.7 7.7 20.0 1
KG-1
CHEMBL612264
IC50 7.7 7.7 20.0 1
PC-9
CHEMBL614102
IC50 7.52 7.52 30.0 1
Rec1
CHEMBL4483266
IC50 7.52 7.52 30.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
CHEMBL5543
IC50 6.46 6.46 350.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.23 6.23 584.0 1
Cyclin-dependent kinase 16
CHEMBL4597
IC50 6.22 6.22 605.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.15 6.15 706.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 5.98 5.98 1050.0 1
Cyclin-dependent kinase 17
CHEMBL5790
IC50 5.82 5.82 1500.0 1
CDK2/Cyclin A2
CHEMBL3038469
IC50 5.46 5.46 3460.0 1
Cyclin-dependent kinase 14
CHEMBL6162
IC50 5.46 5.46 3450.0 1
Cyclin-dependent kinase 18
CHEMBL5316
IC50 5.31 5.31 4900.0 1
A549
CHEMBL392
IC50 5.24 5.24 5780.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK9/Cyclin K IC50 = 2.0 nM 8.7 Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK e... 32129996
MV4-11 IC50 = 3.0 nM 8.52 Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by ce... 39178382
Cyclin-dependent kinase 9 IC50 = 3.57 nM 8.45 Inhibition of CDK9 (unknown origin) using ULight 4EBP1 peptide as substrate incu... 39140066
CDK9/cyclin T1 IC50 = 3.75 nM 8.43 CDK9 Biochemical Assay: To each well of a 96-well plate was added 5× kinase assa... -
Cyclin-dependent kinase 9 IC50 = 4.1 nM 8.39 Inhibition of CDK9 (unknown origin) using ULight 4EBP1 peptide as substrate incu... 39178382
CESS IC50 = 10.0 nM 8.0 Antiproliferative activity against human CESS cells incubated for 72 hrs by cell... 39178382
KG-1 IC50 = 20.0 nM 7.7 Antiproliferative activity against human KG-1 cells incubated for 72 hrs by cell... 39178382
HT-29 IC50 = 20.0 nM 7.7 Antiproliferative activity against human HT-29 cells incubated for 72 hrs by cel... 39178382
Rec1 IC50 = 30.0 nM 7.52 Antiproliferative activity against human REC1 cells incubated for 72 hrs by cell... 39178382
PC-9 IC50 = 30.0 nM 7.52 Antiproliferative activity against human PC-9 cells incubated for 72 hrs by cell... 39178382
Dual specificity tyrosine-phosphorylation-regulated kinase 1B IC50 = 350.0 nM 6.46 Inhibition of DYRK1B (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 1 IC50 = 584.0 nM 6.23 Inhibition of CDK1 (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 16 IC50 = 605.0 nM 6.22 Inhibition of CDK16 (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 2 IC50 = 706.0 nM 6.15 Inhibition of CDK2 (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 5 IC50 = 1050.0 nM 5.98 Inhibition of CDK5 (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 17 IC50 = 1500.0 nM 5.82 Inhibition of CDK17 (unknown origin) by Kinomescan method 35814933
CDK2/Cyclin A2 IC50 = 3460.0 nM 5.46 Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 ... 32129996
Cyclin-dependent kinase 14 IC50 = 3450.0 nM 5.46 Inhibition of CDK14 (unknown origin) by Kinomescan method 35814933
Cyclin-dependent kinase 18 IC50 = 4900.0 nM 5.31 Inhibition of CDK18 (unknown origin) by Kinomescan method 35814933
A549 IC50 = 5780.0 nM 5.24 Antiproliferative activity against human A549 cells incubated for 72 hrs by cell... 39178382

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 U2OS 9
- 10.6019/CHEMBL5303304 Fibroblast 9
- 10.6019/CHEMBL5303304 HEK-293T 8
39178382 10.1021/acs.jmedchem.4c00837 MV4-11 2
35814933 10.1039/d2md00040g Cyclin-dependent kinase 9 2
35814933 10.1039/d2md00040g Cyclin-dependent kinase 2 1
39178382 10.1021/acs.jmedchem.4c00837 ZR-75-1 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 16 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 14 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 8 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 7 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 5 1
32129996 10.1021/acs.jmedchem.9b02121 CDK6/cyclin D3 1
35814933 10.1039/d2md00040g Cyclin-dependent kinase 1 1
35235745 10.1021/acs.jmedchem.1c02190 Cyclin-dependent kinase 9 1
32129996 10.1021/acs.jmedchem.9b02121 L02 1
32129996 10.1021/acs.jmedchem.9b02121 MCF7 1
32129996 10.1021/acs.jmedchem.9b02121 Jurkat 1
32129996 10.1021/acs.jmedchem.9b02121 MDA-MB-231 1
32129996 10.1021/acs.jmedchem.9b02121 CDK2/Cyclin A2 1

Data from ChEMBL 36 via Core Engine