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Assay Detail

CHEMBL1099771

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

Binding
Displacement of [3H]prazosin from human Alpha-1D adrenergic receptor expressed in CHO cells
19
Total Activities
19
Compounds Tested
2
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

Alpha-1D adrenergic receptor (CHEMBL223)
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 7.61 8.89
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 8.89
CHEMBL1078773 1 8.20
CHEMBL1083182 1 8.18
CHEMBL1078953 1 8.17
CHEMBL1082862 1 8.03
CHEMBL1083181 1 7.94
CHEMBL1086156 1 7.69
CHEMBL1084658 1 7.59
CHEMBL1088072 1 7.30
CHEMBL1077168 1 7.24
CHEMBL1087942 1 6.74
CHEMBL1078772 1 6.48
CHEMBL1079066 1 6.45
CHEMBL56 8-OH-DPAT 1 -
CHEMBL1078750 1 -
CHEMBL1078751 1 -
CHEMBL1078954 1 -
CHEMBL1079065 1 -
CHEMBL1088071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 1.288 nM 8.89
CHEMBL1078773 Ki = 6.31 nM 8.20
CHEMBL1083182 Ki = 6.607 nM 8.18
CHEMBL1078953 Ki = 6.761 nM 8.17
CHEMBL1082862 Ki = 9.333 nM 8.03
CHEMBL1083181 Ki = 11.48 nM 7.94
CHEMBL1086156 Ki = 20.42 nM 7.69
CHEMBL1084658 Ki = 25.7 nM 7.59
CHEMBL1088072 Ki = 50.12 nM 7.30
CHEMBL1077168 Ki = 57.54 nM 7.24
CHEMBL1087942 Ki = 181.97 nM 6.74
CHEMBL1078772 Ki = 331.13 nM 6.48
CHEMBL1079066 Ki = 354.81 nM 6.45
CHEMBL56 8-OH-DPAT Ki > 1000.0 nM -
CHEMBL1078750 Ki > 1000.0 nM -
CHEMBL1078751 Ki > 1000.0 nM -
CHEMBL1078954 Ki > 1000.0 nM -
CHEMBL1079065 Ki > 1000.0 nM -
CHEMBL1088071 pKi - -