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Assay Detail

CHEMBL618918

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

Binding
Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor (5-HT 3 receptor) of rat cortex and hippocampus tissue
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 6 — Multiple protein complex / RNA
Curated By Intermediate

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Cappelli A, Anzini M, Vomero S, Canullo L, Mennuni L, Makovec F, Doucet E, Hamon M, Menziani MC, De Benedetti PG, Bruni G, Romeo MR, Giorgi G, Donati A.
J Med Chem (1999) 42 : 1556 -1575
PubMed 10229626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.84 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43355 1 9.64
CHEMBL41841 1 9.22
CHEMBL41511 1 9.22
CHEMBL289664 1 9.15
CHEMBL289486 1 9.05
CHEMBL43512 1 8.74
CHEMBL290065 1 8.72
CHEMBL39081 1 8.62
CHEMBL3707024 1 8.52
CHEMBL289732 1 8.44
CHEMBL3707025 1 8.41
CHEMBL289794 1 8.39
CHEMBL417706 1 8.38
CHEMBL41598 1 8.27
CHEMBL43304 1 8.06
CHEMBL288643 1 7.92
CHEMBL288497 1 7.80
CHEMBL290472 1 7.70
CHEMBL38843 1 7.54
CHEMBL43305 1 7.54
CHEMBL41140 6-NITROQUIPAZINE 1 7.24
CHEMBL3707026 1 7.11
CHEMBL41379 1 7.10
CHEMBL41256 1 6.31
CHEMBL41414 1 5.96
CHEMBL38814 1 5.64
CHEMBL290087 1 5.57
CHEMBL289384 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43355 Ki = 0.23 nM 9.64
CHEMBL41841 Ki = 0.6 nM 9.22
CHEMBL41511 Ki = 0.6 nM 9.22
CHEMBL289664 Ki = 0.7 nM 9.15
CHEMBL289486 Ki = 0.9 nM 9.05
CHEMBL43512 Ki = 1.8 nM 8.74
CHEMBL290065 Ki = 1.9 nM 8.72
CHEMBL39081 Ki = 2.4 nM 8.62
CHEMBL3707024 Ki = 3.0 nM 8.52
CHEMBL289732 Ki = 3.6 nM 8.44
CHEMBL3707025 Ki = 3.9 nM 8.41
CHEMBL289794 Ki = 4.1 nM 8.39
CHEMBL417706 Ki = 4.2 nM 8.38
CHEMBL41598 Ki = 5.4 nM 8.27
CHEMBL43304 Ki = 8.8 nM 8.06
CHEMBL288643 Ki = 12.0 nM 7.92
CHEMBL288497 Ki = 16.0 nM 7.80
CHEMBL290472 Ki = 20.0 nM 7.70
CHEMBL38843 Ki = 29.0 nM 7.54
CHEMBL43305 Ki = 29.0 nM 7.54
CHEMBL41140 6-NITROQUIPAZINE Ki = 58.0 nM 7.24
CHEMBL3707026 Ki = 78.0 nM 7.11
CHEMBL41379 Ki = 80.0 nM 7.10
CHEMBL41256 Ki = 490.0 nM 6.31
CHEMBL41414 Ki = 1100.0 nM 5.96
CHEMBL38814 Ki = 2300.0 nM 5.64
CHEMBL290087 Ki = 2700.0 nM 5.57
CHEMBL289384 Ki = 4900.0 nM 5.31