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Assay Detail

CHEMBL4842092

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

Binding
Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL ↗
99
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Subcellular Membrane
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
Ki 99 7.01 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105760 BREXPIPRAZOLE 4.0 2 9.29
CHEMBL2028019 CARIPRAZINE 4.0 2 8.84
CHEMBL1112 ARIPIPRAZOLE 4.0 2 8.67
CHEMBL54 HALOPERIDOL 4.0 2 8.20
CHEMBL4863832 — — 2 8.18
CHEMBL4862770 — — 2 7.94
CHEMBL4875081 — — 2 7.89
CHEMBL4857759 — — 2 7.81
CHEMBL4862890 — — 2 7.68
CHEMBL4874021 — — 2 7.59
CHEMBL4864436 — — 2 7.56
CHEMBL4876116 — — 2 7.52
CHEMBL4852808 — — 2 7.49
CHEMBL4846472 — — 2 7.48
CHEMBL4859410 — — 2 7.42
CHEMBL4872467 — — 2 7.37
CHEMBL4852524 — — 2 7.36
CHEMBL4862439 — — 2 7.31
CHEMBL4872548 — — 2 7.22
CHEMBL4862301 — — 2 7.21
CHEMBL4877827 — — 2 7.02
CHEMBL4848451 — — 2 7.01
CHEMBL4871762 — — 2 6.90
CHEMBL4863992 — — 2 6.90
CHEMBL4859080 — — 2 6.89
CHEMBL4850635 — — 2 6.81
CHEMBL4865118 — — 2 6.80
CHEMBL4859567 — — 2 6.75
CHEMBL4855583 — — 2 6.67
CHEMBL4871774 — — 2 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105760 BREXPIPRAZOLE Ki = 0.51 nM 9.29
CHEMBL2105760 BREXPIPRAZOLE Ki = 0.5129 nM 9.29
CHEMBL2028019 CARIPRAZINE Ki = 1.45 nM 8.84
CHEMBL2028019 CARIPRAZINE Ki = 1.445 nM 8.84
CHEMBL1112 ARIPIPRAZOLE Ki = 2.13 nM 8.67
CHEMBL1112 ARIPIPRAZOLE Ki = 2.138 nM 8.67
CHEMBL54 HALOPERIDOL Ki = 6.31 nM 8.20
CHEMBL54 HALOPERIDOL Ki = 6.33 nM 8.20
CHEMBL4863832 — Ki = 6.58 nM 8.18
CHEMBL4863832 — Ki = 6.607 nM 8.18
CHEMBL4862770 — Ki = 11.5 nM 7.94
CHEMBL4862770 — Ki = 11.48 nM 7.94
CHEMBL4875081 — Ki = 12.88 nM 7.89
CHEMBL4875081 — Ki = 12.8 nM 7.89
CHEMBL4857759 — Ki = 15.49 nM 7.81
CHEMBL4857759 — Ki = 15.6 nM 7.81
CHEMBL4862890 — Ki = 20.89 nM 7.68
CHEMBL4862890 — Ki = 20.8 nM 7.68
CHEMBL4874021 — Ki = 25.8 nM 7.59
CHEMBL4874021 — Ki = 25.7 nM 7.59
CHEMBL4864436 — Ki = 27.54 nM 7.56
CHEMBL4864436 — Ki = 27.4 nM 7.56
CHEMBL4876116 — Ki = 30.1 nM 7.52
CHEMBL4876116 — Ki = 30.2 nM 7.52
CHEMBL4852808 — Ki = 32.36 nM 7.49
CHEMBL4852808 — Ki = 32.2 nM 7.49
CHEMBL4846472 — Ki = 32.9 nM 7.48
CHEMBL4846472 — Ki = 33.11 nM 7.48
CHEMBL4859410 — Ki = 38.02 nM 7.42
CHEMBL4859410 — Ki = 38.0 nM 7.42
CHEMBL4872467 — Ki = 42.66 nM 7.37
CHEMBL4872467 — Ki = 42.7 nM 7.37
CHEMBL4852524 — Ki = 43.8 nM 7.36
CHEMBL4852524 — Ki = 43.65 nM 7.36
CHEMBL4862439 — Ki = 48.98 nM 7.31
CHEMBL4862439 — Ki = 49.3 nM 7.31
CHEMBL4872548 — Ki = 59.9 nM 7.22
CHEMBL4872548 — Ki = 60.26 nM 7.22
CHEMBL4862301 — Ki = 61.9 nM 7.21
CHEMBL4862301 — Ki = 61.66 nM 7.21
CHEMBL4877827 — Ki = 95.2 nM 7.02
CHEMBL4877827 — Ki = 95.5 nM 7.02
CHEMBL4848451 — Ki = 97.72 nM 7.01
CHEMBL4848451 — Ki = 98.3 nM 7.01
CHEMBL4871762 — Ki = 125.89 nM 6.90
CHEMBL4871762 — Ki = 126.7 nM 6.90
CHEMBL4863992 — Ki = 125.89 nM 6.90
CHEMBL4863992 — Ki = 125.7 nM 6.90
CHEMBL4859080 — Ki = 128.82 nM 6.89
CHEMBL4859080 — Ki = 128.1 nM 6.89