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Assay Detail

CHEMBL4008742

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Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL ↗
46
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234) ↗
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 46 7.49 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071240 — — 2 9.52
CHEMBL4073068 — — 1 9.14
CHEMBL4070196 — — 2 9.04
CHEMBL4100634 — — 1 8.92
CHEMBL4081780 — — 2 8.85
CHEMBL4099798 — — 2 8.64
CHEMBL4072282 — — 2 8.59
CHEMBL4091498 — — 2 8.21
CHEMBL4086944 — — 2 8.04
CHEMBL465 DRONABINOL 4.0 1 7.99
CHEMBL4092052 — — 2 7.85
CHEMBL4069565 — — 2 7.82
CHEMBL4065510 — — 2 7.70
CHEMBL4094794 — — 2 7.28
CHEMBL4099236 — — 2 7.17
CHEMBL4103339 — — 2 7.16
CHEMBL4090459 — — 2 7.03
CHEMBL4102620 — — 2 6.96
CHEMBL4098174 — — 2 6.66
CHEMBL4062484 — — 2 6.47
CHEMBL4072140 — — 2 6.43
CHEMBL4092900 — — 2 6.42
CHEMBL4082631 — — 1 6.18
CHEMBL4079093 — — 2 5.82
CHEMBL4071121 — — 2 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071240 — EC50 = 0.302 nM 9.52
CHEMBL4073068 — EC50 = 0.73 nM 9.14
CHEMBL4071240 — EC50 = 0.9 nM 9.05
CHEMBL4070196 — EC50 = 0.912 nM 9.04
CHEMBL4100634 — EC50 = 1.2 nM 8.92
CHEMBL4081780 — EC50 = 1.413 nM 8.85
CHEMBL4081780 — EC50 = 1.4 nM 8.85
CHEMBL4099798 — EC50 = 2.291 nM 8.64
CHEMBL4099798 — EC50 = 2.3 nM 8.64
CHEMBL4072282 — EC50 = 2.6 nM 8.59
CHEMBL4072282 — EC50 = 2.63 nM 8.58
CHEMBL4091498 — EC50 = 6.166 nM 8.21
CHEMBL4091498 — EC50 = 6.1 nM 8.21
CHEMBL4086944 — EC50 = 9.2 nM 8.04
CHEMBL4086944 — EC50 = 9.12 nM 8.04
CHEMBL465 DRONABINOL EC50 = 10.2 nM 7.99
CHEMBL4070196 — EC50 = 14.0 nM 7.85
CHEMBL4092052 — EC50 = 14.13 nM 7.85
CHEMBL4092052 — EC50 = 14.0 nM 7.85
CHEMBL4069565 — EC50 = 15.14 nM 7.82
CHEMBL4069565 — EC50 = 15.0 nM 7.82
CHEMBL4065510 — EC50 = 19.95 nM 7.70
CHEMBL4065510 — EC50 = 20.0 nM 7.70
CHEMBL4094794 — EC50 = 52.48 nM 7.28
CHEMBL4094794 — EC50 = 52.0 nM 7.28
CHEMBL4099236 — EC50 = 67.61 nM 7.17
CHEMBL4103339 — EC50 = 70.0 nM 7.16
CHEMBL4103339 — EC50 = 70.79 nM 7.15
CHEMBL4090459 — EC50 = 93.33 nM 7.03
CHEMBL4090459 — EC50 = 93.0 nM 7.03
CHEMBL4102620 — EC50 = 109.65 nM 6.96
CHEMBL4102620 — EC50 = 110.0 nM 6.96
CHEMBL4098174 — EC50 = 220.0 nM 6.66
CHEMBL4098174 — EC50 = 218.78 nM 6.66
CHEMBL4099236 — EC50 = 320.0 nM 6.50
CHEMBL4062484 — EC50 = 340.0 nM 6.47
CHEMBL4062484 — EC50 = 338.84 nM 6.47
CHEMBL4072140 — EC50 = 371.54 nM 6.43
CHEMBL4072140 — EC50 = 370.0 nM 6.43
CHEMBL4092900 — EC50 = 380.19 nM 6.42
CHEMBL4092900 — EC50 = 380.0 nM 6.42
CHEMBL4082631 — EC50 = 667.0 nM 6.18
CHEMBL4079093 — EC50 = 1500.0 nM 5.82
CHEMBL4079093 — EC50 = 1513.56 nM 5.82
CHEMBL4071121 — EC50 = 2300.0 nM 5.64
CHEMBL4071121 — EC50 = 2344.23 nM 5.63