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Compound Detail

CHEMBL278780

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O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL278780
Phase Preclinical
Structure Type MOL
InChI Key MCGQZPBZSRMELE-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

767.4
MW (Da)
7.12
ALogP
5
HBA
6
HBD
153.4
PSA (Ų)
0.07
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H51ClN6O5
MW 767.37
Aromatic Rings 4
Heavy Atoms 55
NP-Likeness -0.61

Activity Summary

IC50 4 meas. best 7.12
EC50 1 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholecystokinin receptor type A
CHEMBL2871
IC50 7.12 6.97 75.0 2
Rattus norvegicus
CHEMBL376
EC50 6.32 6.32 480.0 1
Gastrin/cholecystokinin type B receptor
CHEMBL2854
IC50 5.44 5.095 3600.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10866391 10.1016/s0960-894x(00)00198-0 Cholecystokinin receptor type A 1
10866391 10.1016/s0960-894x(00)00198-0 Gastrin/cholecystokinin type B receptor 1
10866391 10.1016/s0960-894x(00)00198-0 Rattus norvegicus 1
10866391 10.1016/s0960-894x(00)00198-0 Jurkat 1
- 10.1016/S0960-894X(00)80687-3 Cholecystokinin receptor type A 1
- 10.1016/S0960-894X(00)80687-3 Gastrin/cholecystokinin type B receptor 1
- 10.1016/S0960-894X(00)80687-3 Unchecked 1

Data from ChEMBL 36 via Core Engine