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Compound Detail

CHEMBL2370110

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CC(C)C[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)C[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC1=O

Basic Information

ChEMBL ID CHEMBL2370110
Phase Preclinical
Structure Type MOL
InChI Key HQMGUCSNMWQMAM-ZKQHQRMCSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

1235.5
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C61H86N16O12
MW 1235.46

Activity Summary

IC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.17 6.17 676.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 808.0 ng.hr.mL-1 Mus musculus
CL 0.001 ml/hr Mus musculus
Cmax 675.05 nM Mus musculus
T1/2 0.5 hr Mus musculus
Tmax 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 676.08 nM 6.17 Displacement of [125I]-Tyr6, His5 from human LHRH1 receptor expressed in HEK 293... 23127987

Literature References

Data from ChEMBL 36 via Core Engine