Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL616569

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

Binding
Binding affinity to displace [3H]2-(di-N-propylamino)-8-hydroxy-tetralin from 5-hydroxytryptamine 1A (5-HT1A) receptor in rat frontal cortex homogenates
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-affinity relationship studies on 5-HT1A receptor ligands. 2. Heterobicyclic phenylpiperazines with N4-aralkyl substituents.
van Steen BJ, van Wijngaarden I, Tulp MT, Soudijn W.
J Med Chem (1994) 37 : 2761 -2773
PubMed 8064803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 8.49 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555633 1 9.82
CHEMBL92242 1 9.70
CHEMBL543851 1 9.60
CHEMBL81728 1 9.52
CHEMBL543139 1 9.49
CHEMBL545720 1 9.43
CHEMBL93421 1 9.36
CHEMBL543141 1 9.34
CHEMBL538273 1 9.33
CHEMBL27457 1 9.30
CHEMBL27558 1 9.27
CHEMBL285158 1 9.21
CHEMBL542671 1 9.17
CHEMBL542906 1 9.14
CHEMBL26834 1 9.09
CHEMBL545722 1 9.07
CHEMBL545721 1 9.02
CHEMBL541077 1 9.00
CHEMBL94115 1 9.00
CHEMBL543377 1 8.85
CHEMBL26988 1 8.77
CHEMBL26601 1 8.66
CHEMBL543138 1 8.40
CHEMBL96595 1 8.24
CHEMBL280825 1 8.23
CHEMBL27655 1 8.11
CHEMBL26355 1 8.10
CHEMBL286287 1 8.09
CHEMBL554093 1 7.96
CHEMBL28288 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555633 Ki = 0.15 nM 9.82
CHEMBL92242 Ki = 0.2 nM 9.70
CHEMBL543851 Ki = 0.25 nM 9.60
CHEMBL81728 Ki = 0.3 nM 9.52
CHEMBL543139 Ki = 0.32 nM 9.49
CHEMBL545720 Ki = 0.37 nM 9.43
CHEMBL93421 Ki = 0.44 nM 9.36
CHEMBL543141 Ki = 0.46 nM 9.34
CHEMBL538273 Ki = 0.47 nM 9.33
CHEMBL27457 Ki = 0.5 nM 9.30
CHEMBL27558 Ki = 0.54 nM 9.27
CHEMBL285158 Ki = 0.61 nM 9.21
CHEMBL542671 Ki = 0.67 nM 9.17
CHEMBL542906 Ki = 0.73 nM 9.14
CHEMBL26834 Ki = 0.81 nM 9.09
CHEMBL545722 Ki = 0.85 nM 9.07
CHEMBL545721 Ki = 0.95 nM 9.02
CHEMBL541077 Ki = 1.0 nM 9.00
CHEMBL94115 Ki = 1.0 nM 9.00
CHEMBL543377 Ki = 1.4 nM 8.85
CHEMBL26988 Ki = 1.7 nM 8.77
CHEMBL26601 Ki = 2.2 nM 8.66
CHEMBL543138 Ki = 4.0 nM 8.40
CHEMBL96595 Ki = 5.8 nM 8.24
CHEMBL280825 Ki = 5.9 nM 8.23
CHEMBL27655 Ki = 7.7 nM 8.11
CHEMBL26355 Ki = 8.0 nM 8.10
CHEMBL286287 Ki = 8.1 nM 8.09
CHEMBL554093 Ki = 11.0 nM 7.96
CHEMBL28288 Ki = 12.0 nM 7.92
CHEMBL61032 Ki = 13.0 nM 7.89
CHEMBL416382 Ki = 20.0 nM 7.70
CHEMBL542184 Ki = 22.0 nM 7.66
CHEMBL329246 Ki = 23.0 nM 7.64
CHEMBL27694 Ki = 24.0 nM 7.62
CHEMBL92745 Ki = 28.0 nM 7.55
CHEMBL26645 Ki = 29.0 nM 7.54
CHEMBL282614 ELTOPRAZINE Ki = 40.0 nM 7.40
CHEMBL26819 Ki = 56.0 nM 7.25
CHEMBL28110 Ki = 64.0 nM 7.19
CHEMBL96658 Ki = 64.0 nM 7.19
CHEMBL26905 Ki = 66.0 nM 7.18
CHEMBL27590 Ki = 80.0 nM 7.10