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

CHEMBL4582951

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
CN(C)C/C=C/C(=O)Nc1ccc(C(=O)N[C@@]2(C)CCC[C@@H](Nc3ncc(Cl)c(-c4c[nH]c5ccccc45)n3)C2)nc1

Basic Information

ChEMBL ID CHEMBL4582951
Phase Preclinical
Structure Type MOL
InChI Key SCJNYBYSTCRPAO-LXBQGUBHSA-N
8
Targets
17
Activities
3
Assay Types
3
PK Parameters
18
Publications
0
Known Names

Molecular Properties

587.1
MW (Da)
5.27
ALogP
7
HBA
4
HBD
127.9
PSA (Ų)
0.20
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H35ClN8O2
MW 587.13
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.76

Activity Summary

IC50 14 meas. best 7.7
EC50 2 meas. best 8.1
Ki 1 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HL-60
CHEMBL383
EC50 8.1 8.1 8.0 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
EC50 7.89 7.89 13.0 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
Ki 7.76 7.76 17.4 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 7.7 7.158 20.0 5
CDK12/Cyclin K
CHEMBL4106169
IC50 7.7 7.7 20.0 1
Cyclin-dependent kinase 7
CHEMBL3055
IC50 7.1 5.59 80.0 2
Cyclin-dependent kinase 12
CHEMBL3559692
IC50 6.7 6.695 200.0 2
CDK9/cyclin T1
CHEMBL2111389
IC50 6.04 6.04 914.0 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 6.04 6.04 910.0 2
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.67 5.67 2117.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 6.0 mL.min-1.kg-1 Mus musculus
CL 5.6 mL.min-1.kg-1 Mus musculus
CL 5.6 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HL-60 EC50 = 8.0 nM 8.1 Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Gl... 31477350
CDK7/Cyclin H/MNAT1 EC50 = 13.0 nM 7.89 Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin) 31477350
CDK7/Cyclin H/MNAT1 Ki = 17.4 nM 7.76 Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin) using ... 31477350
CDK7/Cyclin H/MNAT1 IC50 = 20.0 nM 7.7 Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) in leukemia cells 36561076
CDK7/Cyclin H/MNAT1 IC50 = 20.0 nM 7.7 Inhibition of CDK7/Cyclin H/MNAT1 (unknown origin) using 5-FAM-YSPTSPSYSPTSPSYSP... 32707525
CDK12/Cyclin K IC50 = 20.0 nM 7.7 Competitive irreversible inhibition of CDK12/cyclinK (unknown origin) in presenc... 31477350
Cyclin-dependent kinase 7 IC50 = 80.0 nM 7.1 Inhibition of CDK7 (unknown origin) 38852339
CDK7/Cyclin H/MNAT1 IC50 = 84.0 nM 7.08 Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin) using ... 31477350
CDK7/Cyclin H/MNAT1 IC50 = 84.0 nM 7.08 Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins f... 32150405
Cyclin-dependent kinase 12 IC50 = 200.0 nM 6.7 Inhibition of CDK12 (unknown origin) 38852339
Cyclin-dependent kinase 12 IC50 = 204.0 nM 6.69 Inhibition of CDK12 (unknown origin) 32150405
CDK7/Cyclin H/MNAT1 IC50 = 590.0 nM 6.23 Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin) using ... 31477350
CDK9/cyclin T1 IC50 = 914.0 nM 6.04 Competitive irreversible inhibition of CDK9/cyclin T (unknown origin) in presenc... 31477350
Cyclin-dependent kinase 9 IC50 = 914.0 nM 6.04 Inhibition of CDK9 (unknown origin) 32150405
Cyclin-dependent kinase 9 IC50 = 910.0 nM 6.04 Inhibition of CDK9 (unknown origin) 38852339
Cyclin-dependent kinase 2 IC50 = 2117.0 nM 5.67 Inhibition of CDK2 (unknown origin) 32150405
Cyclin-dependent kinase 7 IC50 = 84000.0 nM 4.08 Inhibition of CDK7 (unknown origin) incubated for 5 to 60 mins in presence of AT... 35235745

Literature References

PubMed DOI Target Context # Activities
31477350 10.1016/j.bmcl.2019.126637 CDK7/Cyclin H/MNAT1 6
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 7 1
38852339 10.1016/j.ejmech.2024.116547 Cyclin-dependent kinase 9 1
38852339 10.1016/j.ejmech.2024.116547 Cyclin-dependent kinase 12 1
38852339 10.1016/j.ejmech.2024.116547 Cyclin-dependent kinase 7 1
32707525 10.1016/j.ejmech.2020.112571 CDK7/Cyclin H/MNAT1 1
35235745 10.1021/acs.jmedchem.1c02190 ADMET 1
35235745 10.1021/acs.jmedchem.1c02190 Cyclin-dependent kinase 7 1
36561076 10.1039/d2md00216g CDK7/Cyclin H/MNAT1 1
32150405 10.1021/acs.jmedchem.9b01985 CDK7/Cyclin H/MNAT1 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 12 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 9 1
32150405 10.1021/acs.jmedchem.9b01985 Cyclin-dependent kinase 2 1
32150405 10.1021/acs.jmedchem.9b01985 ADMET 1
31477350 10.1016/j.bmcl.2019.126637 CDK12/Cyclin K 1
31477350 10.1016/j.bmcl.2019.126637 CDK9/cyclin T1 1
31477350 10.1016/j.bmcl.2019.126637 HL-60 1
31477350 10.1016/j.bmcl.2019.126637 ADMET 1

Data from ChEMBL 36 via Core Engine