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Compound Detail

CHEMBL4225966

SEL-120 FREE BASE
Phase I
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Phase I
Cc1c(Br)c(Br)c2c3c1nc(N1CCNCC1)n3CCC2

Basic Information

ChEMBL ID CHEMBL4225966
Name SEL-120 FREE BASE
Phase Phase I
Structure Type MOL
InChI Key FSBMCTDYWXIBLM-UHFFFAOYSA-N

Known Names

Sel-120 free base
26
Targets
41
Activities
2
Assay Types
18
PK Parameters
20
Publications
1
Known Names

Molecular Properties

414.1
MW (Da)
3.23
ALogP
4
HBA
1
HBD
33.1
PSA (Ų)
0.78
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Extended Properties

Molecular Formula C15H18Br2N4
MW 414.14
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.76

Activity Summary

IC50 39 meas. best 9.01
EC50 2 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 9.01 9.01 1.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 8.87 8.825 1.3 2
Dual specificity protein kinase CLK4
CHEMBL4203
IC50 8.57 8.57 2.7 1
CDK8/Cyclin C
CHEMBL3038474
IC50 8.4 8.0967 4.0 6
Cyclin-dependent kinase 8
CHEMBL5719
IC50 8.36 7.8475 4.4 4
CDK2/Cyclin A2
CHEMBL3038469
IC50 8.33 8.33 4.7 1
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 8.28 8.28 5.3 1
Cyclin-C/Cyclin-dependent kinase 19
CHEMBL3883323
IC50 8.0 7.985 10.0 4
Cyclin-dependent kinase 19
CHEMBL6002
IC50 7.72 7.66 19.1 2
Cyclin-dependent kinase 8/19
CHEMBL3885556
EC50 7.7 7.7 20.0 1
CDK8/CDK19
CHEMBL4888455
EC50 7.7 7.7 20.0 1
Unchecked
CHEMBL612545
IC50 7.69 7.69 20.5 1
Dual specificity protein kinase CLK2
CHEMBL4225
IC50 7.68 7.68 21.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 7.4 7.1 40.0 2
MV4-11
CHEMBL613835
IC50 7.36 6.98 43.8 2
Serine/threonine-protein kinase haspin
CHEMBL1075163
IC50 7.34 7.34 46.0 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 7.29 7.29 51.0 1
Homeodomain-interacting protein kinase 3
CHEMBL4577
IC50 6.88 6.88 131.8 1
Casein kinase II subunit alpha'
CHEMBL4070
IC50 6.55 6.55 278.9 1
Serine/threonine-protein kinase pim-2
CHEMBL4523
IC50 6.53 6.53 298.2 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 6.48 6.48 332.2 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 6.16 6.16 700.0 1
Rho-associated protein kinase 1
CHEMBL3231
IC50 6.14 6.14 717.5 1
Cyclin-dependent kinase 9
CHEMBL3116
IC50 5.97 5.97 1070.0 1
Mitogen-activated protein kinase 15
CHEMBL5198
IC50 5.87 5.87 1344.0 1
Casein kinase I isoform alpha
CHEMBL2793
IC50 5.86 5.86 1390.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1352.0 ng.hr.mL-1 Mus musculus
AUC 56.0 ng.hr.mL-1 Rattus norvegicus
AUC 2056.0 ng.hr.mL-1 Canis lupus familiaris
CL 81.0 mL.min-1.kg-1 Mus musculus
CL 246.0 mL.min-1.kg-1 Rattus norvegicus
CL 30.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 345.29 nM Mus musculus
Cmax 28.98 nM Rattus norvegicus
Cmax 519.15 nM Canis lupus familiaris
F 155.0 % Mus musculus
F 20.0 % Rattus norvegicus
F 136.0 % Canis lupus familiaris
T1/2 3.01 hr Mus musculus
T1/2 1.77 hr Rattus norvegicus
T1/2 2.7 hr Canis lupus familiaris
Tmax 1.3 hr Mus musculus
Tmax 1.67 hr Rattus norvegicus
Tmax 4.18 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2/cyclin E1 IC50 = 0.968 nM 9.01 Inhibition of CDK2/cyclinE1 (unknown origin) by ADP-Glo chemiluminescence assay 38690856
Cyclin-dependent kinase 5/CDK5 activator 1 IC50 = 1.338 nM 8.87 Inhibition of CDK5/p35NCK (unknown origin) by ADP-Glo chemiluminescence assay 38690856
Cyclin-dependent kinase 5/CDK5 activator 1 IC50 = 1.66 nM 8.78 Inhibition of CDK5/p25NCK (unknown origin) by ADP-Glo chemiluminescence assay 38690856
Dual specificity protein kinase CLK4 IC50 = 2.7 nM 8.57 Inhibition of CLK4 (unknown origin) by ADP-Glo assay 38690856
CDK8/Cyclin C IC50 = 4.0 nM 8.4 Inhibition of CDK8/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by rad... 29266937
CDK8/Cyclin C IC50 = 4.4 nM 8.36 Inhibition of CDK8/Cyclin C (unknown origin) 35485642
Cyclin-dependent kinase 8 IC50 = 4.4 nM 8.36 Inhibition of CDK8 (unknown origin) 32707525
CDK8/Cyclin C IC50 = 4.4 nM 8.36 Inhibition of CDK8/CyclinC (unknown origin) incubated for 60 mins in presence of... 38690856
CDK2/Cyclin A2 IC50 = 4.701 nM 8.33 Inhibition of CDK2/cyclinA2 (unknown origin) by ADP-Glo chemiluminescence assay 38690856
Dual specificity protein kinase CLK1 IC50 = 5.3 nM 8.28 Inhibition of CLK1 (unknown origin) by ADP-Glo assay 38690856
Cyclin-C/Cyclin-dependent kinase 19 IC50 = 10.0 nM 8.0 Inhibition of CDK19/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by ra... 29266937
Cyclin-C/Cyclin-dependent kinase 19 IC50 = 10.4 nM 7.98 Inhibition of CDK19/CyclinC (unknown origin) incubated for 60 mins in presence o... 38690856
Cyclin-C/Cyclin-dependent kinase 19 IC50 = 10.4 nM 7.98 Inhibition of CDK19/Cyclin C (unknown origin) 35485642
Cyclin-C/Cyclin-dependent kinase 19 IC50 = 10.4 nM 7.98 Inhibition of CDK19/Cyclin C (unknown origin) 32707525
CDK8/Cyclin C IC50 = 14.11 nM 7.85 Inhibition of His tagged human recombinant CDK8/Cyclin C expressed in baculoviru... 37029334
CDK8/Cyclin C IC50 = 14.1 nM 7.85 Displacement of tracer 236 from CDK8/cyclin C (unknown origin) preincubated for ... 38690856
Cyclin-dependent kinase 8 IC50 = 14.5 nM 7.84 Inhibition of CDK8 (unknown origin) by HTRF assay 38690856
CDK8/Cyclin C IC50 = 17.5 nM 7.76 Inhibition of CDK8/CyclinC (unknown origin) by ADP-Glo chemiluminescence assay 38690856
Cyclin-dependent kinase 8 IC50 = 17.5 nM 7.76 Inhibition of CDK8 (unknown origin) by ADP-Glo assay 38690856
Cyclin-dependent kinase 19 IC50 = 19.13 nM 7.72 Inhibition of CDK19 (unknown origin) by HTRF assay 38690856

Literature References

PubMed DOI Target Context # Activities
38690856 10.1021/acs.jmedchem.4c00248 ADMET 24
38690856 10.1021/acs.jmedchem.4c00248 Unchecked 8
29266937 10.1021/acs.jmedchem.7b00901 Unchecked 3
38690856 10.1021/acs.jmedchem.4c00248 CDK8/Cyclin C 3
37029334 10.1021/acs.jmedchem.2c01718 MV4-11 2
38690856 10.1021/acs.jmedchem.4c00248 Cyclin-dependent kinase 5/CDK5 activator 1 2
38690856 10.1021/acs.jmedchem.4c00248 Cyclin-dependent kinase 8 2
38690856 10.1021/acs.jmedchem.4c00248 Cyclin-dependent kinase 19 2
38690856 10.1021/acs.jmedchem.4c00248 Cytochrome P450 1A2 2
35485642 10.1021/acs.jmedchem.1c02064 Cyclin-C/Cyclin-dependent kinase 19 1
36889252 10.1016/j.ejmech.2023.115214 A-375 1
36889252 10.1016/j.ejmech.2023.115214 MDA-MB-231 1
38690856 10.1021/acs.jmedchem.4c00248 Cyclin-C/Cyclin-dependent kinase 19 1
36889252 10.1016/j.ejmech.2023.115214 Cyclin-dependent kinase 8 1
32707525 10.1016/j.ejmech.2020.112571 Cyclin-C/Cyclin-dependent kinase 19 1
32707525 10.1016/j.ejmech.2020.112571 Cyclin-dependent kinase 8 1
29266937 10.1021/acs.jmedchem.7b00901 Cyclin-C/Cyclin-dependent kinase 19 1
29266937 10.1021/acs.jmedchem.7b00901 OCI-AML-3 1
29266937 10.1021/acs.jmedchem.7b00901 MV4-11 1
29266937 10.1021/acs.jmedchem.7b00901 HL-60 1

Data from ChEMBL 36 via Core Engine