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Compound Detail

CHEMBL1958337

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Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NN2C

Basic Information

ChEMBL ID CHEMBL1958337
Phase Preclinical
Structure Type MOL
InChI Key UYIVCPRWMLOCSB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

323.8
MW (Da)
3.43
ALogP
5
HBA
0
HBD
46.3
PSA (Ų)
0.69
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14ClN5
MW 323.79
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.20

Activity Summary

Kd 1 meas. best 6.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 4
CHEMBL1163125
Kd 6.19 6.19 640.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bromodomain-containing protein 4 Kd = 640.0 nM 6.19 Binding affinity to BRD4-BD1 by isothermal titration calorimetry 22137933

Literature References

PubMed DOI Target Context # Activities
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 4 6
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 2 4
22137933 10.1016/j.bmc.2011.10.080 Bromodomain-containing protein 3 4
22137933 10.1016/j.bmc.2011.10.080 Bromodomain testis-specific protein 2
22137933 10.1016/j.bmc.2011.10.080 Bromodomain adjacent to zinc finger domain protein 2B 2
22137933 10.1016/j.bmc.2011.10.080 CREB-binding protein 2
22137933 10.1016/j.bmc.2011.10.080 Unchecked 2
22137933 10.1016/j.bmc.2011.10.080 Protein polybromo-1 2
22137933 10.1016/j.bmc.2011.10.080 Histone acetyltransferase KAT2B 2

Data from ChEMBL 36 via Core Engine