Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4842095

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

Functional
Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL ↗
91
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

2-Phenylcyclopropylmethylamine Derivatives as Dopamine D<sub>2</sub> Receptor Partial Agonists: Design, Synthesis, and Biological Evaluation.
Yan W, Fan L, Yu J, Liu R, Wang H, Tan L, Wang S, Cheng J.
J Med Chem (2021) 64 : 17239 -17258
PubMed 34797051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 91 7.73 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852524 — — 2 8.73
CHEMBL4872467 — — 2 8.70
CHEMBL2028019 CARIPRAZINE 4.0 2 8.63
CHEMBL4862770 — — 2 8.60
CHEMBL4862890 — — 2 8.44
CHEMBL4865118 — — 2 8.39
CHEMBL4857759 — — 2 8.35
CHEMBL4863832 — — 2 8.33
CHEMBL4862439 — — 2 8.29
CHEMBL4874021 — — 2 8.17
CHEMBL4850635 — — 2 8.15
CHEMBL4877827 — — 2 8.13
CHEMBL4875081 — — 2 8.08
CHEMBL4864369 — — 2 8.02
CHEMBL4863992 — — 2 8.00
CHEMBL4859410 — — 2 7.97
CHEMBL4855583 — — 2 7.88
CHEMBL4865389 — — 2 7.85
CHEMBL4864436 — — 2 7.83
CHEMBL4852835 — — 2 7.83
CHEMBL4846472 — — 2 7.82
CHEMBL240773 QUINPIROLE 2.0 2 7.80
CHEMBL2105760 BREXPIPRAZOLE 4.0 2 7.79
CHEMBL4852808 — — 2 7.73
CHEMBL1112 ARIPIPRAZOLE 4.0 2 7.72
CHEMBL4849780 — — 2 7.66
CHEMBL4859567 — — 2 7.63
CHEMBL4859080 — — 2 7.56
CHEMBL4871762 — — 2 7.53
CHEMBL4872548 — — 2 7.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852524 — EC50 = 1.86 nM 8.73
CHEMBL4852524 — EC50 = 1.95 nM 8.71
CHEMBL4872467 — EC50 = 2.02 nM 8.70
CHEMBL2028019 CARIPRAZINE EC50 = 2.344 nM 8.63
CHEMBL2028019 CARIPRAZINE EC50 = 2.37 nM 8.62
CHEMBL4872467 — EC50 = 2.512 nM 8.60
CHEMBL4862770 — EC50 = 2.512 nM 8.60
CHEMBL4862770 — EC50 = 2.5 nM 8.60
CHEMBL4862890 — EC50 = 3.631 nM 8.44
CHEMBL4862890 — EC50 = 3.63 nM 8.44
CHEMBL4865118 — EC50 = 4.074 nM 8.39
CHEMBL4865118 — EC50 = 4.06 nM 8.39
CHEMBL4857759 — EC50 = 4.467 nM 8.35
CHEMBL4857759 — EC50 = 4.47 nM 8.35
CHEMBL4863832 — EC50 = 4.66 nM 8.33
CHEMBL4863832 — EC50 = 4.677 nM 8.33
CHEMBL4862439 — EC50 = 5.08 nM 8.29
CHEMBL4862439 — EC50 = 5.754 nM 8.24
CHEMBL4874021 — EC50 = 6.75 nM 8.17
CHEMBL4874021 — EC50 = 6.761 nM 8.17
CHEMBL4850635 — EC50 = 7.079 nM 8.15
CHEMBL4850635 — EC50 = 7.08 nM 8.15
CHEMBL4877827 — EC50 = 7.413 nM 8.13
CHEMBL4877827 — EC50 = 7.43 nM 8.13
CHEMBL4875081 — EC50 = 8.318 nM 8.08
CHEMBL4875081 — EC50 = 8.3 nM 8.08
CHEMBL4864369 — EC50 = 9.49 nM 8.02
CHEMBL4864369 — EC50 = 9.55 nM 8.02
CHEMBL4863992 — EC50 = 10.0 nM 8.00
CHEMBL4863992 — EC50 = 10.0 nM 8.00
CHEMBL4859410 — EC50 = 10.72 nM 7.97
CHEMBL4859410 — EC50 = 11.0 nM 7.96
CHEMBL4855583 — EC50 = 13.18 nM 7.88
CHEMBL4855583 — EC50 = 13.1 nM 7.88
CHEMBL4865389 — EC50 = 14.13 nM 7.85
CHEMBL4865389 — EC50 = 14.1 nM 7.85
CHEMBL4864436 — EC50 = 14.9 nM 7.83
CHEMBL4852835 — EC50 = 14.79 nM 7.83
CHEMBL4852835 — EC50 = 14.7 nM 7.83
CHEMBL4864436 — EC50 = 14.79 nM 7.83
CHEMBL4846472 — EC50 = 15.14 nM 7.82
CHEMBL4846472 — EC50 = 15.0 nM 7.82
CHEMBL240773 QUINPIROLE EC50 = 15.85 nM 7.80
CHEMBL240773 QUINPIROLE EC50 = 15.7 nM 7.80
CHEMBL2105760 BREXPIPRAZOLE EC50 = 16.22 nM 7.79
CHEMBL2105760 BREXPIPRAZOLE EC50 = 16.1 nM 7.79
CHEMBL4852808 — EC50 = 18.62 nM 7.73
CHEMBL4852808 — EC50 = 18.8 nM 7.73
CHEMBL1112 ARIPIPRAZOLE EC50 = 19.05 nM 7.72
CHEMBL1112 ARIPIPRAZOLE EC50 = 18.9 nM 7.72