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Assay Detail

CHEMBL995093

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

Binding
Displacement of [3H]ketanserin from 5HT2 receptor in pig striatal membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Striatum
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Dörfler M, Tschammer N, Hamperl K, Hübner H, Gmeiner P.
J Med Chem (2008) 51 : 6829 -6838
PubMed 18834111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.62 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484358 1 6.34
CHEMBL484204 1 6.10
CHEMBL444128 1 6.07
CHEMBL485227 1 6.05
CHEMBL483593 1 5.85
CHEMBL484202 1 5.57
CHEMBL491466 1 5.24
CHEMBL484357 1 5.08
CHEMBL485384 1 5.08
CHEMBL484203 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484358 Ki = 460.0 nM 6.34
CHEMBL484204 Ki = 790.0 nM 6.10
CHEMBL444128 Ki = 860.0 nM 6.07
CHEMBL485227 Ki = 890.0 nM 6.05
CHEMBL483593 Ki = 1400.0 nM 5.85
CHEMBL484202 Ki = 2700.0 nM 5.57
CHEMBL491466 Ki = 5700.0 nM 5.24
CHEMBL484357 Ki = 8300.0 nM 5.08
CHEMBL485384 Ki = 8300.0 nM 5.08
CHEMBL484203 Ki = 15000.0 nM 4.82