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Compound Detail

CHEMBL3422012

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Cc1nc(-c2nnc3n2CCN(C(=O)c2ccc(-c4cccs4)cc2)C3)cs1

Basic Information

ChEMBL ID CHEMBL3422012
Phase Preclinical
Structure Type MOL
InChI Key SSHIUOSPXKCYNW-UHFFFAOYSA-N
7
Targets
19
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
4.09
ALogP
7
HBA
0
HBD
63.9
PSA (Ų)
0.51
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17N5OS2
MW 407.52
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -2.04

Activity Summary

IC50 11 meas. best 7.1
Ki 8 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuromedin-K receptor
CHEMBL4429
IC50 7.1 7.0867 79.4 3
Neuromedin-K receptor
CHEMBL4429
Ki 7.1 7.0825 79.4 8
Cytochrome P450 2C19
CHEMBL3622
IC50 4.82 4.82 15000.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.72 4.72 19000.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.72 4.72 19000.0 1
Transcriptional regulator ERG
CHEMBL1293191
IC50 4.58 4.58 26000.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.58 4.5767 26000.0 3
Cytochrome P450 3A4
CHEMBL340
IC50 4.52 4.52 30000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuromedin-K receptor IC50 = 79.43 nM 7.1 Antagonist activity at recombinant human NK3R expressed in CHO cells assessed as... 25738882
Neuromedin-K receptor Ki = 79.43 nM 7.1 Displacement of [3H]-SB222200 from recombinant human NK3R expressed in CHO cell ... 25738882
Neuromedin-K receptor IC50 = 83.0 nM 7.08 Aequorin Functional Assay: Changes in intracellular calcium levels are a recogni... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Binding Competition Assay: NK3: The ability of compounds of the invention to inh... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Binding Competition Assay: NK3: The ability of compounds of the invention to inh... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Competitive Binding Assay: NK3: The ability of compounds of the invention to inh... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Competitive Binding Assay: NK3: The ability of compounds of the invention to inh... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 3H-SB222200 Binding Competition Assay with Human NK-3 Receptor: The ability of c... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Aequorin Assay with Human NK-3 Receptor: The antagonist activity of compounds of... -
Neuromedin-K receptor Ki = 83.0 nM 7.08 Binding Competition Assay: The ability of compounds of the invention to inhibit ... -
Neuromedin-K receptor IC50 = 83.0 nM 7.08 Aequorin Assay with Human NK-3 Receptor: The antagonist activity of compounds of... -
Cytochrome P450 2C19 IC50 = 15000.0 nM 4.82 Inhibition of CYP2C19 (unknown origin) by luciferase reporter assay in presence ... 25738882
Cytochrome P450 1A2 IC50 = 19000.0 nM 4.72 Inhibition of CYP1A2 (unknown origin) by luciferase reporter assay in presence o... 25738882
Cytochrome P450 2C9 IC50 = 19000.0 nM 4.72 Inhibition of CYP2C9 (unknown origin) by luciferase reporter assay in presence o... 25738882
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 26000.0 nM 4.58 Inhibiton Assay : hERG: The hERG inhibition study aims at quantifying the in vit... -
Transcriptional regulator ERG IC50 = 26000.0 nM 4.58 hERG Inhibition Assay: The human Ether-a-go-go Related Gene (hERG) encodes the i... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 26000.0 nM 4.58 Inhibition Assay: The hERG inhibition study aims at quantifying the in vitro eff... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 27000.0 nM 4.57 Inhibition of human ERG expressed in HEK293 cells after 5 mins by patch-clamp as... 25738882
Cytochrome P450 3A4 IC50 = 30000.0 nM 4.52 Inhibition of CYP3A4 (unknown origin) by luciferase reporter assay in presence o... 25738882

Literature References

PubMed DOI Target Context # Activities
25738882 10.1021/jm5017413 Neuromedin-K receptor 2
25738882 10.1021/jm5017413 No relevant target 2
25738882 10.1021/jm5017413 Cytochrome P450 3A4 1
25738882 10.1021/jm5017413 Cytochrome P450 2D6 1
25738882 10.1021/jm5017413 Cytochrome P450 2C9 1
25738882 10.1021/jm5017413 Cytochrome P450 2C19 1
25738882 10.1021/jm5017413 Cytochrome P450 1A2 1
25738882 10.1021/jm5017413 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine