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Assay Detail

CHEMBL671591

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

Binding
Binding affinity against dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand.
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
Yasunaga T, Kimura T, Naito R, Kontani T, Wanibuchi F, Yamashita H, Nomura T, Tsukamoto S, Yamaguchi T, Mase T.
J Med Chem (1998) 41 : 2765 -2778
PubMed 9667967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.97 9.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96279 1 9.83
CHEMBL25213 1 9.59
CHEMBL419147 1 9.54
CHEMBL96222 1 9.51
CHEMBL96714 3 9.32
CHEMBL96546 1 8.64
CHEMBL96517 1 8.52
CHEMBL95044 1 8.52
CHEMBL92651 1 8.30
CHEMBL96578 1 8.09
CHEMBL318418 1 8.04
CHEMBL96858 1 7.93
CHEMBL319575 1 7.63
CHEMBL96901 1 7.62
CHEMBL93503 1 7.60
CHEMBL96265 1 7.49
CHEMBL94957 1 7.46
CHEMBL96435 1 7.42
CHEMBL96266 1 7.41
CHEMBL94317 1 7.38
CHEMBL330714 1 7.36
CHEMBL318417 1 7.30
CHEMBL329675 1 7.26
CHEMBL93030 1 7.21
CHEMBL96903 1 7.15
CHEMBL94428 1 6.96
CHEMBL317532 1 6.82
CHEMBL316593 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96279 Ki = 0.149 nM 9.83
CHEMBL25213 Ki = 0.259 nM 9.59
CHEMBL419147 Ki = 0.288 nM 9.54
CHEMBL96222 Ki = 0.312 nM 9.51
CHEMBL96714 Ki = 0.482 nM 9.32
CHEMBL96714 Ki = 0.724 nM 9.14
CHEMBL96546 Ki = 2.31 nM 8.64
CHEMBL96517 Ki = 2.99 nM 8.52
CHEMBL95044 Ki = 3.02 nM 8.52
CHEMBL96714 Ki = 4.11 nM 8.39
CHEMBL92651 Ki = 4.98 nM 8.30
CHEMBL96578 Ki = 8.13 nM 8.09
CHEMBL318418 Ki = 9.07 nM 8.04
CHEMBL96858 Ki = 11.7 nM 7.93
CHEMBL319575 Ki = 23.3 nM 7.63
CHEMBL96901 Ki = 23.7 nM 7.62
CHEMBL93503 Ki = 25.1 nM 7.60
CHEMBL96265 Ki = 32.3 nM 7.49
CHEMBL94957 Ki = 34.6 nM 7.46
CHEMBL96435 Ki = 38.0 nM 7.42
CHEMBL96266 Ki = 38.8 nM 7.41
CHEMBL94317 Ki = 42.1 nM 7.38
CHEMBL330714 Ki = 43.9 nM 7.36
CHEMBL318417 Ki = 49.6 nM 7.30
CHEMBL329675 Ki = 55.1 nM 7.26
CHEMBL93030 Ki = 62.3 nM 7.21
CHEMBL96903 Ki = 70.4 nM 7.15
CHEMBL94428 Ki = 111.0 nM 6.96
CHEMBL317532 Ki = 153.0 nM 6.82
CHEMBL316593 Ki = 1540.0 nM 5.81