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Compound Detail

CHEMBL286835

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Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCSCc4csc(C=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1

Basic Information

ChEMBL ID CHEMBL286835
Phase Preclinical
Structure Type MOL
InChI Key LOQFTNBNQJALJO-UMSFTDKQSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

755.9
MW (Da)
4.55
ALogP
11
HBA
6
HBD
206.2
PSA (Ų)
0.10
QED
3
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H41N9O5S2
MW 755.93
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness -1.15

Activity Summary

Kd 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL4654
Kd 5.7 5.7 1995.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor Kd = 1995.26 nM 5.7 Antagonistic activity by inhibition histamine H2 receptor from rats. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(96)00249-1 Gastrin/cholecystokinin type B receptor 2
- 10.1016/S0960-894X(96)00249-1 Cholecystokinin receptor type A 1
- 10.1016/S0960-894X(96)00249-1 Cholecystokinin receptor 1
- 10.1016/S0960-894X(96)00249-1 Histamine H2 receptor 1

Data from ChEMBL 36 via Core Engine