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Assay Detail

CHEMBL4701870

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Agonist activity at human NTS1 expressed in HEK293 cells co-expressing Galphaq/RlucII/GFP10-Ggamma1/Gbeta1 assessed as increase in Galphaq activation incubated for 10 mins in presence of coelenterazine 400A by BRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 1 (CHEMBL4123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Gonzalez S,Dumitrascuta M,Eiselt E,Louis S,Kunze L,Blasiol A,Vivancos M,Previti S,Dewolf E,Martin C,Tourwé D,Cavelier F,Gendron L,Sarret P,Spetea M,Ballet S
J Med Chem (2020) 63 : 12929 -12941
PubMed 32902268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.53 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415788 1 9.82
CHEMBL4789659 1 9.62
CHEMBL4744531 1 9.59
CHEMBL4776986 1 9.07
CHEMBL4798887 1 8.89
CHEMBL4597094 1 8.77
CHEMBL4749016 1 8.74
CHEMBL4758754 1 8.41
CHEMBL4745899 1 8.17
CHEMBL4747286 1 7.82
CHEMBL4761165 1 7.72
CHEMBL4742666 1 5.72
CHEMBL4750783 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415788 EC50 = 0.15 nM 9.82
CHEMBL4789659 EC50 = 0.24 nM 9.62
CHEMBL4744531 EC50 = 0.26 nM 9.59
CHEMBL4776986 EC50 = 0.86 nM 9.07
CHEMBL4798887 EC50 = 1.3 nM 8.89
CHEMBL4597094 EC50 = 1.7 nM 8.77
CHEMBL4749016 EC50 = 1.8 nM 8.74
CHEMBL4758754 EC50 = 3.9 nM 8.41
CHEMBL4745899 EC50 = 6.7 nM 8.17
CHEMBL4747286 EC50 = 15.0 nM 7.82
CHEMBL4761165 EC50 = 19.1 nM 7.72
CHEMBL4742666 EC50 = 1900.0 nM 5.72
CHEMBL4750783 EC50 - -