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Compound Detail

CHEMBL4442620

RONICICLIB
🧪 Phase II
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🧪 Phase II
C[C@@H](O)[C@@H](C)Oc1nc(Nc2ccc(S(=N)(=O)C3CC3)cc2)ncc1C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4442620
Name RONICICLIB
Phase Phase II
Structure Type MOL
InChI Key UELYDGOOJPRWGF-MFOHZAOFSA-N

Known Names

Bay 1000394 Bay-1000394 BAY10-00394 BAY1000394 Roniciclib
16
Targets
58
Activities
1
Assay Types
0
PK Parameters
20
Publications
5
Known Names
3
Indications
1
Mechanisms

Molecular Properties

430.4
MW (Da)
3.96
ALogP
7
HBA
3
HBD
108.2
PSA (Ų)
0.61
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -ciclib

Extended Properties

Molecular Formula C18H21F3N4O3S
MW 430.45
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.85

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Cyclin-dependent kinase inhibitor INHIBITOR Cyclin-dependent kinase

Indications

Neoplasms Small Cell Lung Carcinoma Carcinoma, Non-Small-Cell Lung

Activity Summary

IC50 58 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 8.3 8.3 5.0 4
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.3 8.0857 5.0 7
Cyclin-dependent kinase 7
CHEMBL3055
IC50 8.3 7.8333 5.0 3
Cyclin-dependent kinase 1
CHEMBL308
IC50 8.3 8.1571 5.0 7
Cyclin-dependent kinase 9
CHEMBL3116
IC50 8.3 8.2583 5.0 6
Cyclin-dependent kinase 4
CHEMBL331
IC50 8.3 8.0214 5.0 7
Cyclin-dependent kinase 3
CHEMBL4442
IC50 8.3 8.175 5.0 2
Cyclin-dependent kinase 1/cyclin B1
CHEMBL1907602
IC50 8.15 8.15 7.0 4
Unchecked
CHEMBL612545
IC50 8.15 8.1 7.0 2
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 8.05 8.05 9.0 3
CDK3/Cyclin E
CHEMBL3038471
IC50 8.05 8.05 9.0 1
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 7.96 7.96 11.0 4
MCF7
CHEMBL387
IC50 7.82 7.8133 15.0 3
Cyclin-dependent kinase 7/ cyclin H
CHEMBL2111288
IC50 7.6 7.6 25.0 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 7.6 7.6 25.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.79 6.79 163.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK9/cyclin T1 IC50 = 5.0 nM 8.3 Inhibition of recombinant human full-length C-terminal His6-tagged CDK9/human fu... 30543440
CDK9/cyclin T1 IC50 = 5.0 nM 8.3 Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T... 27171036
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 Inhibition of CDK9 (unknown origin) 37234044
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 Inhibition of CDK9 (unknown origin) 36332552
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 Inhibition of CDK9 (unknown origin) 35235745
CDK9/cyclin T1 IC50 = 5.0 nM 8.3 Inhibition of CDK9/Cyclin T1 (unknown origin) 35485642
Cyclin-dependent kinase 1 IC50 = 5.0 nM 8.3 Inhibition of CDK1 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 2 IC50 = 5.0 nM 8.3 Inhibition of CDK2 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 3 IC50 = 5.0 nM 8.3 Inhibition of CDK3 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 4 IC50 = 5.0 nM 8.3 Inhibition of CDK4 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 7 IC50 = 5.0 nM 8.3 Inhibition of CDK7 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 Inhibition of CDK9 (unknown origin) expressed in baculovirus-infected Sf9 insect... 33356242
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 Inhibition of CDK9 (unknown origin) 32866383
CDK9/cyclin T1 IC50 = 5.0 nM 8.3 Inhibition of CDK9/Cyclin T1 (unknown origin) 30639897
Cyclin-dependent kinase 1/cyclin B1 IC50 = 7.0 nM 8.15 Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 resi... 30543440
Cyclin-dependent kinase 1 IC50 = 7.0 nM 8.15 Inhibition of CDK1 (unknown origin) 38564299
Cyclin-dependent kinase 1 IC50 = 7.0 nM 8.15 Inhibition of CDK1 (unknown origin) 37234044
Cyclin-dependent kinase 1 IC50 = 7.0 nM 8.15 Inhibition of CDK1 (unknown origin) 36332552
Cyclin-dependent kinase 1 IC50 = 7.0 nM 8.15 Inhibition of CDK1 (unknown origin) 35235745
Cyclin-dependent kinase 1 IC50 = 7.0 nM 8.15 Inhibition of CDK1 (unknown origin) 32866383

Literature References

PubMed DOI Target Context # Activities
35485642 10.1021/acs.jmedchem.1c02064 Unchecked 2
27171036 10.1021/acs.jmedchem.6b00150 Cyclin-dependent kinase 5/CDK5 activator 1 1
38564299 10.1021/acs.jmedchem.4c00312 CDK7/Cyclin H/MNAT1 1
30639897 10.1016/j.ejmech.2019.01.003 Cyclin-dependent kinase 1/cyclin B1 1
30543440 10.1021/acs.jmedchem.8b01469 CDK7/Cyclin H/MNAT1 1
30543440 10.1021/acs.jmedchem.8b01469 Cyclin-dependent kinase 1/cyclin B1 1
30543440 10.1021/acs.jmedchem.8b01469 CDK3/Cyclin E 1
30543440 10.1021/acs.jmedchem.8b01469 Cyclin-dependent kinase 4/cyclin D1 1
30543440 10.1021/acs.jmedchem.8b01469 CDK9/cyclin T1 1
30543440 10.1021/acs.jmedchem.8b01469 Cyclin-dependent kinase 2/cyclin E1 1
30543440 10.1021/acs.jmedchem.8b01469 Cyclin-dependent kinase 5/CDK5 activator 1 1
26115571 10.1016/j.bmcl.2015.05.100 Cyclin-dependent kinase 1/cyclin B1 1
27171036 10.1021/acs.jmedchem.6b00150 CDK9/cyclin T1 1
27171036 10.1021/acs.jmedchem.6b00150 Cyclin-dependent kinase 4/cyclin D1 1
27171036 10.1021/acs.jmedchem.6b00150 Cyclin-dependent kinase 1/cyclin B1 1
27171036 10.1021/acs.jmedchem.6b00150 Cyclin-dependent kinase 2/cyclin E1 1
27171036 10.1021/acs.jmedchem.6b00150 CDK7/Cyclin H/MNAT1 1
26115571 10.1016/j.bmcl.2015.05.100 Carbonic anhydrase 2 1
26115571 10.1016/j.bmcl.2015.05.100 MCF7 1
26115571 10.1016/j.bmcl.2015.05.100 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine