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Assay Detail

CHEMBL4677471

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

Binding
Displacement of [3H]-spiperone from recombinant human D2L receptor expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.
Xu JW,Qi YL,Wu JW,Yuan RX,Chen XW,Li JQ
Bioorg Med Chem Lett (2021) 31 : 127681 -127681
PubMed 33189775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.70 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028019 CARIPRAZINE 4.0 1 9.31
CHEMBL4759975 1 8.55
CHEMBL4741702 1 8.54
CHEMBL4752414 1 8.24
CHEMBL4799863 1 8.23
CHEMBL4797996 1 8.20
CHEMBL4756826 1 8.01
CHEMBL4753808 1 7.92
CHEMBL4762024 1 7.85
CHEMBL4745809 1 7.69
CHEMBL4750939 1 7.62
CHEMBL4741673 1 7.60
CHEMBL4784751 1 7.50
CHEMBL4788140 1 7.36
CHEMBL4761274 1 7.08
CHEMBL4743651 1 7.04
CHEMBL4780335 1 7.03
CHEMBL4762918 1 7.00
CHEMBL4755563 1 6.72
CHEMBL4779912 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028019 CARIPRAZINE Ki = 0.49 nM 9.31
CHEMBL4759975 Ki = 2.8 nM 8.55
CHEMBL4741702 Ki = 2.9 nM 8.54
CHEMBL4752414 Ki = 5.8 nM 8.24
CHEMBL4799863 Ki = 5.9 nM 8.23
CHEMBL4797996 Ki = 6.3 nM 8.20
CHEMBL4756826 Ki = 9.8 nM 8.01
CHEMBL4753808 Ki = 12.1 nM 7.92
CHEMBL4762024 Ki = 14.1 nM 7.85
CHEMBL4745809 Ki = 20.6 nM 7.69
CHEMBL4750939 Ki = 23.9 nM 7.62
CHEMBL4741673 Ki = 25.3 nM 7.60
CHEMBL4784751 Ki = 31.6 nM 7.50
CHEMBL4788140 Ki = 43.7 nM 7.36
CHEMBL4761274 Ki = 84.0 nM 7.08
CHEMBL4743651 Ki = 91.1 nM 7.04
CHEMBL4780335 Ki = 93.9 nM 7.03
CHEMBL4762918 Ki = 99.3 nM 7.00
CHEMBL4755563 Ki = 188.7 nM 6.72
CHEMBL4779912 Ki = 290.5 nM 6.54