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Assay Detail

CHEMBL4842093

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 Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL ↗
89
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 89 7.75 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 2 8.99
CHEMBL4846472 — — 2 8.58
CHEMBL4877827 — — 2 8.54
CHEMBL240773 QUINPIROLE 2.0 2 8.52
CHEMBL4875081 — — 2 8.47
CHEMBL4864436 — — 2 8.46
CHEMBL4863832 — — 2 8.39
CHEMBL4862439 — — 2 8.38
CHEMBL4874021 — — 2 8.38
CHEMBL4852808 — — 2 8.38
CHEMBL4859410 — — 2 8.17
CHEMBL4857759 — — 2 8.11
CHEMBL4864369 — — 2 8.07
CHEMBL4862770 — — 2 8.05
CHEMBL4863992 — — 2 8.03
CHEMBL4862890 — — 2 8.03
CHEMBL2105760 BREXPIPRAZOLE 4.0 2 8.00
CHEMBL4872467 — — 2 7.96
CHEMBL4850635 — — 2 7.95
CHEMBL1112 ARIPIPRAZOLE 4.0 2 7.91
CHEMBL4852524 — — 2 7.89
CHEMBL4859080 — — 2 7.83
CHEMBL4865118 — — 2 7.78
CHEMBL4871762 — — 2 7.75
CHEMBL4861553 — — 2 7.72
CHEMBL4855775 — — 2 7.64
CHEMBL4872548 — — 2 7.58
CHEMBL4859567 — — 2 7.58
CHEMBL4871833 — — 2 7.46
CHEMBL4862301 — — 2 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE EC50 = 1.023 nM 8.99
CHEMBL2028019 CARIPRAZINE EC50 = 1.02 nM 8.99
CHEMBL4846472 — EC50 = 2.63 nM 8.58
CHEMBL4846472 — EC50 = 2.63 nM 8.58
CHEMBL4877827 — EC50 = 2.88 nM 8.54
CHEMBL4877827 — EC50 = 2.884 nM 8.54
CHEMBL240773 QUINPIROLE EC50 = 2.99 nM 8.52
CHEMBL240773 QUINPIROLE EC50 = 3.02 nM 8.52
CHEMBL4875081 — EC50 = 3.388 nM 8.47
CHEMBL4875081 — EC50 = 3.41 nM 8.47
CHEMBL4864436 — EC50 = 3.47 nM 8.46
CHEMBL4864436 — EC50 = 3.467 nM 8.46
CHEMBL4863832 — EC50 = 4.074 nM 8.39
CHEMBL4852808 — EC50 = 4.169 nM 8.38
CHEMBL4863832 — EC50 = 4.12 nM 8.38
CHEMBL4874021 — EC50 = 4.169 nM 8.38
CHEMBL4874021 — EC50 = 4.21 nM 8.38
CHEMBL4862439 — EC50 = 4.169 nM 8.38
CHEMBL4862439 — EC50 = 4.22 nM 8.38
CHEMBL4852808 — EC50 = 4.15 nM 8.38
CHEMBL4859410 — EC50 = 6.761 nM 8.17
CHEMBL4859410 — EC50 = 6.8 nM 8.17
CHEMBL4857759 — EC50 = 7.762 nM 8.11
CHEMBL4857759 — EC50 = 7.82 nM 8.11
CHEMBL4864369 — EC50 = 8.45 nM 8.07
CHEMBL4864369 — EC50 = 8.511 nM 8.07
CHEMBL4862770 — EC50 = 8.913 nM 8.05
CHEMBL4862770 — EC50 = 8.9 nM 8.05
CHEMBL4862890 — EC50 = 9.333 nM 8.03
CHEMBL4862890 — EC50 = 9.43 nM 8.03
CHEMBL4863992 — EC50 = 9.333 nM 8.03
CHEMBL4863992 — EC50 = 9.3 nM 8.03
CHEMBL2105760 BREXPIPRAZOLE EC50 = 10.0 nM 8.00
CHEMBL2105760 BREXPIPRAZOLE EC50 = 10.2 nM 7.99
CHEMBL4872467 — EC50 = 10.96 nM 7.96
CHEMBL4872467 — EC50 = 10.9 nM 7.96
CHEMBL4850635 — EC50 = 11.22 nM 7.95
CHEMBL4850635 — EC50 = 11.2 nM 7.95
CHEMBL1112 ARIPIPRAZOLE EC50 = 12.3 nM 7.91
CHEMBL1112 ARIPIPRAZOLE EC50 = 12.4 nM 7.91
CHEMBL4852524 — EC50 = 12.88 nM 7.89
CHEMBL4852524 — EC50 = 12.9 nM 7.89
CHEMBL4859080 — EC50 = 14.79 nM 7.83
CHEMBL4859080 — EC50 = 14.73 nM 7.83
CHEMBL4865118 — EC50 = 16.6 nM 7.78
CHEMBL4865118 — EC50 = 16.7 nM 7.78
CHEMBL4871762 — EC50 = 17.8 nM 7.75
CHEMBL4871762 — EC50 = 17.78 nM 7.75
CHEMBL4861553 — EC50 = 19.05 nM 7.72
CHEMBL4861553 — EC50 = 18.9 nM 7.72