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Assay Detail

CHEMBL1043963

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity.
Zhang J, Zhang H, Cai W, Yu L, Zhen X, Zhang A.
Bioorg Med Chem (2009) 17 : 4873 -4880
PubMed 19559623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.65 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574595 1 7.07
CHEMBL574623 1 7.01
CHEMBL574700 1 6.98
CHEMBL585740 1 6.88
CHEMBL582945 1 6.88
CHEMBL585741 1 6.63
CHEMBL572490 1 6.42
CHEMBL585742 1 6.34
CHEMBL574627 1 6.19
CHEMBL575203 1 6.10
CHEMBL574558 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574595 Ki = 85.0 nM 7.07
CHEMBL574623 Ki = 98.0 nM 7.01
CHEMBL574700 Ki = 105.0 nM 6.98
CHEMBL585740 Ki = 133.0 nM 6.88
CHEMBL582945 Ki = 133.0 nM 6.88
CHEMBL585741 Ki = 235.0 nM 6.63
CHEMBL572490 Ki = 381.0 nM 6.42
CHEMBL585742 Ki = 457.0 nM 6.34
CHEMBL574627 Ki = 648.0 nM 6.19
CHEMBL575203 Ki = 799.0 nM 6.10
CHEMBL574558 Ki > 1000.0 nM -