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Assay Detail

CHEMBL907458

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

Binding
Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
Cuisiat S, Bourdiol N, Lacharme V, Newman-Tancredi A, Colpaert F, Vacher B.
J Med Chem (2007) 50 : 865 -876
PubMed 17300168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.86 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384657 1 9.02
CHEMBL56 8-OH-DPAT 1 8.85
CHEMBL375297 1 8.77
CHEMBL220808 SARIZOTAN 3.0 1 8.65
CHEMBL221692 ADOPRAZINE 2.0 1 8.64
CHEMBL221920 1 8.44
CHEMBL221131 1 8.26
CHEMBL218261 1 8.24
CHEMBL218313 1 8.21
CHEMBL219486 1 8.02
CHEMBL221743 1 7.91
CHEMBL413777 1 7.78
CHEMBL441546 1 7.68
CHEMBL221957 1 7.64
CHEMBL218217 1 7.58
CHEMBL220809 1 7.53
CHEMBL386988 1 7.46
CHEMBL221183 1 7.37
CHEMBL425810 1 7.33
CHEMBL219111 1 7.21
CHEMBL218166 BIFEPRUNOX 3.0 1 7.19
CHEMBL376634 1 7.17
CHEMBL54 HALOPERIDOL 4.0 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384657 Ki = 0.955 nM 9.02
CHEMBL56 8-OH-DPAT Ki = 1.413 nM 8.85
CHEMBL375297 Ki = 1.698 nM 8.77
CHEMBL220808 SARIZOTAN Ki = 2.239 nM 8.65
CHEMBL221692 ADOPRAZINE Ki = 2.291 nM 8.64
CHEMBL221920 Ki = 3.631 nM 8.44
CHEMBL221131 Ki = 5.495 nM 8.26
CHEMBL218261 Ki = 5.754 nM 8.24
CHEMBL218313 Ki = 6.166 nM 8.21
CHEMBL219486 Ki = 9.55 nM 8.02
CHEMBL221743 Ki = 12.3 nM 7.91
CHEMBL413777 Ki = 16.6 nM 7.78
CHEMBL441546 Ki = 20.89 nM 7.68
CHEMBL221957 Ki = 22.91 nM 7.64
CHEMBL218217 Ki = 26.3 nM 7.58
CHEMBL220809 Ki = 29.51 nM 7.53
CHEMBL386988 Ki = 34.67 nM 7.46
CHEMBL221183 Ki = 42.66 nM 7.37
CHEMBL425810 Ki = 46.77 nM 7.33
CHEMBL219111 Ki = 61.66 nM 7.21
CHEMBL218166 BIFEPRUNOX Ki = 64.57 nM 7.19
CHEMBL376634 Ki = 67.61 nM 7.17
CHEMBL54 HALOPERIDOL Ki = 1698.24 nM 5.77