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Compound Detail

CHEMBL182600

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O=C1CC[C@](CCN2CC(N3CCC(F)CC3)C2)(c2ccc(Cl)c(Cl)c2)CN1CC1CCC(F)(F)CC1

Basic Information

ChEMBL ID CHEMBL182600
Phase Preclinical
Structure Type MOL
InChI Key WNKRABSIBSPIHJ-HHHXNRCGSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

560.5
MW (Da)
6.19
ALogP
3
HBA
0
HBD
26.8
PSA (Ų)
0.40
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H38Cl2F3N3O
MW 560.53
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 9.4
Kd 1 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-K receptor
CHEMBL2327
IC50 9.4 9.4 0.4 1
Substance-K receptor
CHEMBL2327
Kd 9.2 9.2 0.6 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-K receptor IC50 = 0.3981 nM 9.4 Inhibition of human Neurokinin 2 receptor 16039119
Substance-K receptor Kd = 0.631 nM 9.2 pA2 for NK2 receptor of human bladder IM9 cells 16039119

Literature References

PubMed DOI Target Context # Activities
16039119 10.1016/j.bmcl.2005.05.134 Substance-K receptor 2
16039119 10.1016/j.bmcl.2005.05.134 Homo sapiens 2
16039119 10.1016/j.bmcl.2005.05.134 No relevant target 1
16039119 10.1016/j.bmcl.2005.05.134 ADMET 1
16039119 10.1016/j.bmcl.2005.05.134 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine