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Assay Detail

CHEMBL616072

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

Binding
Binding affinity against 5-hydroxytryptamine 1A receptor on rat hippocampus using [3H]8-OH-DPAT as radioligand.
34
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
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 34 8.15 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419147 1 9.80
CHEMBL96578 1 9.73
CHEMBL25213 1 9.66
CHEMBL96222 1 9.57
CHEMBL96714 3 9.51
CHEMBL96279 1 9.36
CHEMBL96517 1 8.63
CHEMBL93503 1 8.59
CHEMBL94317 1 8.57
CHEMBL93030 1 8.51
CHEMBL96435 1 8.39
CHEMBL318417 1 8.38
CHEMBL95044 1 8.13
CHEMBL96546 1 8.05
CHEMBL92651 1 8.02
CHEMBL96903 1 7.96
CHEMBL329675 1 7.75
CHEMBL318418 1 7.74
CHEMBL96266 1 7.74
CHEMBL96265 1 7.72
CHEMBL313420 1 7.71
CHEMBL96901 1 7.62
CHEMBL96858 1 7.56
CHEMBL94957 1 7.55
CHEMBL330714 1 7.38
CHEMBL94428 1 7.36
CHEMBL92668 1 7.31
CHEMBL95135 1 7.28
CHEMBL319575 1 7.25
CHEMBL316593 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419147 Ki = 0.159 nM 9.80
CHEMBL96578 Ki = 0.188 nM 9.73
CHEMBL25213 Ki = 0.221 nM 9.66
CHEMBL96222 Ki = 0.27 nM 9.57
CHEMBL96714 Ki = 0.31 nM 9.51
CHEMBL96279 Ki = 0.435 nM 9.36
CHEMBL96714 Ki = 0.716 nM 9.14
CHEMBL96714 Ki = 2.1 nM 8.68
CHEMBL96517 Ki = 2.34 nM 8.63
CHEMBL93503 Ki = 2.6 nM 8.59
CHEMBL94317 Ki = 2.67 nM 8.57
CHEMBL93030 Ki = 3.07 nM 8.51
CHEMBL96435 Ki = 4.04 nM 8.39
CHEMBL318417 Ki = 4.19 nM 8.38
CHEMBL95044 Ki = 7.33 nM 8.13
CHEMBL96546 Ki = 8.99 nM 8.05
CHEMBL92651 Ki = 9.53 nM 8.02
CHEMBL96903 Ki = 11.0 nM 7.96
CHEMBL329675 Ki = 18.0 nM 7.75
CHEMBL96266 Ki = 18.4 nM 7.74
CHEMBL318418 Ki = 18.3 nM 7.74
CHEMBL96265 Ki = 19.0 nM 7.72
CHEMBL313420 Ki = 19.3 nM 7.71
CHEMBL96901 Ki = 24.0 nM 7.62
CHEMBL96858 Ki = 27.7 nM 7.56
CHEMBL94957 Ki = 28.3 nM 7.55
CHEMBL330714 Ki = 41.8 nM 7.38
CHEMBL94428 Ki = 43.4 nM 7.36
CHEMBL92668 Ki = 48.8 nM 7.31
CHEMBL95135 Ki = 52.7 nM 7.28
CHEMBL319575 Ki = 55.8 nM 7.25
CHEMBL316593 Ki = 69.0 nM 7.16
CHEMBL94303 Ki = 77.0 nM 7.11
CHEMBL317532 Ki = 680.0 nM 6.17