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Assay Detail

CHEMBL2215842

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

Binding
Displacement of [3H]5-carboxamidotryptamine to human 5HT1A expressed in HEK293 cells by filter binding assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB.
J Med Chem (2011) 54 : 3206 -3221
PubMed 21486038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 6.76 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2205051 1 7.85
CHEMBL49 BUSPIRONE 4.0 1 7.68
CHEMBL2205041 1 7.52
CHEMBL2204357 1 7.51
CHEMBL2204360 1 7.41
CHEMBL2205044 1 7.41
CHEMBL2205045 1 7.36
CHEMBL2205054 1 7.28
CHEMBL2205050 1 7.23
CHEMBL2205035 1 7.19
CHEMBL2204355 1 7.17
CHEMBL2205053 1 7.17
CHEMBL2205043 1 7.16
CHEMBL2204356 1 7.12
CHEMBL2204363 1 7.11
CHEMBL2204359 1 7.11
CHEMBL2204361 1 7.03
CHEMBL2205049 1 7.00
CHEMBL2205033 1 6.92
CHEMBL2205042 1 6.89
CHEMBL2205048 1 6.85
CHEMBL2205052 1 6.80
CHEMBL2204362 1 6.68
CHEMBL2205046 1 6.62
CHEMBL2205034 1 6.51
CHEMBL2204358 1 6.48
CHEMBL2204364 1 6.38
CHEMBL2205032 1 6.27
CHEMBL2205039 1 5.96
CHEMBL2205036 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2205051 Ki = 14.0 nM 7.85
CHEMBL49 BUSPIRONE Ki = 21.0 nM 7.68
CHEMBL2205041 Ki = 30.0 nM 7.52
CHEMBL2204357 Ki = 31.0 nM 7.51
CHEMBL2204360 Ki = 39.0 nM 7.41
CHEMBL2205044 Ki = 39.0 nM 7.41
CHEMBL2205045 Ki = 44.0 nM 7.36
CHEMBL2205054 Ki = 53.0 nM 7.28
CHEMBL2205050 Ki = 59.0 nM 7.23
CHEMBL2205035 Ki = 65.0 nM 7.19
CHEMBL2205053 Ki = 68.0 nM 7.17
CHEMBL2204355 Ki = 68.0 nM 7.17
CHEMBL2205043 Ki = 69.0 nM 7.16
CHEMBL2204356 Ki = 75.0 nM 7.12
CHEMBL2204359 Ki = 78.0 nM 7.11
CHEMBL2204363 Ki = 78.0 nM 7.11
CHEMBL2204361 Ki = 94.0 nM 7.03
CHEMBL2205049 Ki = 100.0 nM 7.00
CHEMBL2205033 Ki = 120.0 nM 6.92
CHEMBL2205042 Ki = 130.0 nM 6.89
CHEMBL2205048 Ki = 140.0 nM 6.85
CHEMBL2205052 Ki = 160.0 nM 6.80
CHEMBL2204362 Ki = 210.0 nM 6.68
CHEMBL2205046 Ki = 240.0 nM 6.62
CHEMBL2205034 Ki = 310.0 nM 6.51
CHEMBL2204358 Ki = 330.0 nM 6.48
CHEMBL2204364 Ki = 420.0 nM 6.38
CHEMBL2205032 Ki = 540.0 nM 6.27
CHEMBL2205036 Ki = 1100.0 nM 5.96
CHEMBL2205039 Ki = 1100.0 nM 5.96
CHEMBL2205031 Ki = 1400.0 nM 5.85
CHEMBL2205047 Ki = 2500.0 nM 5.60
CHEMBL2205038 Ki = 2500.0 nM 5.60
CHEMBL2204365 Ki = 2700.0 nM 5.57
CHEMBL2205040 Ki = 2800.0 nM 5.55
CHEMBL2205037 Ki = 4000.0 nM 5.40
CHEMBL549 CITALOPRAM Ki - -
CHEMBL46 ONDANSETRON Ki - -