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Assay Detail

CHEMBL1099772

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

Binding
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in human HeLa cells
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a new series of 5-HT1A receptor agonists.
Franchini S, Prandi A, Sorbi C, Tait A, Baraldi A, Angeli P, Buccioni M, Cilia A, Poggesi E, Fossa P, Brasili L.
Bioorg Med Chem Lett (2010) 20 : 2017 -2020
PubMed 20185311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.44 9.89
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1086156 1 9.89
CHEMBL1082862 1 9.22
CHEMBL1078953 1 9.05
CHEMBL1083182 1 8.99
CHEMBL13647 BMY-7378 1 8.90
CHEMBL1078773 1 8.77
CHEMBL1078772 1 8.66
CHEMBL1077168 1 8.58
CHEMBL1083181 1 8.45
CHEMBL56 8-OH-DPAT 1 8.43
CHEMBL1079066 1 8.12
CHEMBL1088072 1 8.10
CHEMBL1084658 1 8.08
CHEMBL1078751 1 7.54
CHEMBL1087942 1 7.27
CHEMBL1079065 1 7.01
CHEMBL1078954 1 -
CHEMBL1078750 1 -
CHEMBL1088071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1086156 Ki = 0.1288 nM 9.89
CHEMBL1082862 Ki = 0.6026 nM 9.22
CHEMBL1078953 Ki = 0.8913 nM 9.05
CHEMBL1083182 Ki = 1.023 nM 8.99
CHEMBL13647 BMY-7378 Ki = 1.259 nM 8.90
CHEMBL1078773 Ki = 1.698 nM 8.77
CHEMBL1078772 Ki = 2.188 nM 8.66
CHEMBL1077168 Ki = 2.63 nM 8.58
CHEMBL1083181 Ki = 3.548 nM 8.45
CHEMBL56 8-OH-DPAT Ki = 3.715 nM 8.43
CHEMBL1079066 Ki = 7.586 nM 8.12
CHEMBL1088072 Ki = 7.943 nM 8.10
CHEMBL1084658 Ki = 8.318 nM 8.08
CHEMBL1078751 Ki = 28.84 nM 7.54
CHEMBL1087942 Ki = 53.7 nM 7.27
CHEMBL1079065 Ki = 97.72 nM 7.01
CHEMBL1078954 Ki > 1000.0 nM -
CHEMBL1078750 Ki > 1000.0 nM -
CHEMBL1088071 pKi - -