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Assay Detail

CHEMBL4008740

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

Functional
Agonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assay
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase.
De Simone A, Russo D, Ruda GF, Micoli A, Ferraro M, Di Martino RM, Ottonello G, Summa M, Armirotti A, Bandiera T, Cavalli A, Bottegoni G.
J Med Chem (2017) 60 : 2287 -2304
PubMed 28182408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.44 7.98
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102620 1 7.98
CHEMBL4092052 1 7.89
CHEMBL4070196 1 7.89
CHEMBL4069565 1 7.86
CHEMBL4103339 1 7.83
CHEMBL4072282 1 7.67
CHEMBL4091498 1 7.40
CHEMBL4071240 1 7.35
CHEMBL4094794 1 7.31
CHEMBL4099236 1 7.28
CHEMBL4081780 1 7.27
CHEMBL4099798 1 7.25
CHEMBL4071121 1 7.24
CHEMBL4086944 1 7.18
CHEMBL4079093 1 6.87
CHEMBL4065510 1 6.83
CHEMBL4060896 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102620 EC50 = 10.4 nM 7.98
CHEMBL4092052 EC50 = 13.0 nM 7.89
CHEMBL4070196 EC50 = 13.0 nM 7.89
CHEMBL4069565 EC50 = 13.7 nM 7.86
CHEMBL4103339 EC50 = 14.7 nM 7.83
CHEMBL4072282 EC50 = 21.5 nM 7.67
CHEMBL4091498 EC50 = 39.9 nM 7.40
CHEMBL4071240 EC50 = 45.0 nM 7.35
CHEMBL4094794 EC50 = 49.3 nM 7.31
CHEMBL4099236 EC50 = 53.0 nM 7.28
CHEMBL4081780 EC50 = 54.2 nM 7.27
CHEMBL4099798 EC50 = 56.4 nM 7.25
CHEMBL4071121 EC50 = 57.9 nM 7.24
CHEMBL4086944 EC50 = 66.2 nM 7.18
CHEMBL4079093 EC50 = 135.0 nM 6.87
CHEMBL4065510 EC50 = 147.0 nM 6.83
CHEMBL4060896 Activity - -