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Assay Detail

CHEMBL2445951

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

Binding
Displacement of [3H]way100635 from human recombinant 5HT1A receptor stably expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.
Lewellyn K, Bialonska D, Loria MJ, White SW, Sufka KJ, Zjawiony JK.
Bioorg Med Chem (2013) 21 : 7083 -7090
PubMed 24084296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.58 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2058419 1 6.50
CHEMBL1170237 1 6.28
CHEMBL2058420 1 5.74
CHEMBL2058427 1 5.60
CHEMBL2058416 1 5.58
CHEMBL2058695 1 5.56
CHEMBL1173331 1 5.49
CHEMBL2442275 1 5.46
CHEMBL2058415 1 5.34
CHEMBL2058426 1 5.16
CHEMBL2442277 1 5.14
CHEMBL2442276 1 5.13
CHEMBL2058429 1 -
CHEMBL511879 1 -
CHEMBL2058418 1 -
CHEMBL404232 APLYSINOPSIN 1 -
CHEMBL463249 1 -
CHEMBL2058428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2058419 Ki = 315.0 nM 6.50
CHEMBL1170237 Ki = 527.0 nM 6.28
CHEMBL2058420 Ki = 1812.0 nM 5.74
CHEMBL2058427 Ki = 2513.0 nM 5.60
CHEMBL2058416 Ki = 2624.0 nM 5.58
CHEMBL2058695 Ki = 2753.0 nM 5.56
CHEMBL1173331 Ki = 3215.0 nM 5.49
CHEMBL2442275 Ki = 3445.0 nM 5.46
CHEMBL2058415 Ki = 4608.0 nM 5.34
CHEMBL2058426 Ki = 6927.0 nM 5.16
CHEMBL2442277 Ki = 7269.0 nM 5.14
CHEMBL2442276 Ki = 7361.0 nM 5.13
CHEMBL2058429 Ki > 10000.0 nM -
CHEMBL511879 Ki > 10000.0 nM -
CHEMBL2058418 Ki > 10000.0 nM -
CHEMBL404232 APLYSINOPSIN Ki > 10000.0 nM -
CHEMBL463249 Ki > 10000.0 nM -
CHEMBL2058428 Ki > 10000.0 nM -