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Compound Detail

CHEMBL506126

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CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL506126
Phase Preclinical
Structure Type BOTH
InChI Key PNJXWIJKATVXEY-FAQCDESUSA-N
4
Targets
10
Activities
3
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

1667.0
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C76H127N23O19
MW 1666.99

Activity Summary

EC50 7 meas. best 9.82
IC50 2 meas. best 8.16
Kd 1 meas. best 7.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Parathyroid hormone/parathyroid hormone-related peptide receptor
CHEMBL1793
EC50 9.82 8.6867 0.1 3
Unchecked
CHEMBL612545
EC50 9.7 8.61 0.2 2
Parathyroid hormone/parathyroid hormone-related peptide receptor
CHEMBL6038
EC50 8.96 8.96 1.1 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 8.22 8.22 6.0 1
Parathyroid hormone/parathyroid hormone-related peptide receptor
CHEMBL1793
IC50 8.16 7.71 6.9 2
Parathyroid hormone/parathyroid hormone-related peptide receptor
CHEMBL1793
Kd 7.67 7.67 21.6 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3333 hr Rattus norvegicus
T1/2 0.25 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Parathyroid hormone/parathyroid hormone-related peptide receptor EC50 = 0.15 nM 9.82 Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells ass... 17428923
Unchecked EC50 = 0.2 nM 9.7 Decrease in collagen synthesis in neonatal CD1 mouse calivaria bone assessed as ... 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor EC50 = 1.1 nM 8.96 Activity at rat PTH/PTH-related peptide receptor expressed in rat UMR106 cells a... 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor EC50 = 2.2 nM 8.66 Activity at human PTH/PTH-related peptide receptor expressed in SAOS2 cells asse... 17428923
NON-PROTEIN TARGET EC50 = 6.0 nM 8.22 Stimulation of cell proliferation in neonatal CD1 mouse calivaria assessed as in... 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor IC50 = 6.87 nM 8.16 Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed... 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor Kd = 21.6 nM 7.67 Binding affinity to PTH/PTH-related peptide receptor expressed in HKRK-B28 cells 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor EC50 = 26.0 nM 7.58 Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells ass... 17428923
Unchecked EC50 = 30.0 nM 7.52 Stimulation of osteoclast-mediated bone resorption in fetal Sprague-Dawley rat r... 17428923
Parathyroid hormone/parathyroid hormone-related peptide receptor IC50 = 55.4 nM 7.26 Displacement of [125I]DPC-AJ1951 from PTH/PTH-related peptide receptor expressed... 17428923

Literature References

PubMed DOI Target Context # Activities
17428923 10.1073/pnas.0605125104 Unchecked 21
17428923 10.1073/pnas.0605125104 Parathyroid hormone/parathyroid hormone-related peptide receptor 7
17428923 10.1073/pnas.0605125104 Rattus norvegicus 3
17428923 10.1073/pnas.0605125104 Plasma 1
17428923 10.1073/pnas.0605125104 ADMET 1
17428923 10.1073/pnas.0605125104 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine