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Assay Detail

CHEMBL3299606

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

Binding
Displacement of [125I]BE2254 from human alpha1d receptor expressed in HEK293 cells
17
Total Activities
17
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

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High affinity ligands and potent antagonists for the α1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives.
Romeo G, Salerno L, Pittalà V, Modica MN, Siracusa MA, Materia L, Buccioni M, Marucci G, Minneman KP.
Eur J Med Chem (2014) 83 : 419 -432
PubMed 24992070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.97 10.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3297829 1 10.25
CHEMBL3298750 1 9.85
CHEMBL3298749 1 9.43
CHEMBL220221 1 9.40
CHEMBL3298745 1 9.24
CHEMBL3298023 1 9.12
CHEMBL3298746 1 9.04
CHEMBL3298017 1 9.00
CHEMBL3298748 1 8.93
CHEMBL220781 1 8.90
CHEMBL3298019 1 8.78
CHEMBL3298024 1 8.64
CHEMBL3298747 1 8.49
CHEMBL3298021 1 8.48
CHEMBL3298018 1 8.39
CHEMBL3298020 1 8.30
CHEMBL3298022 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3297829 Ki = 0.05623 nM 10.25
CHEMBL3298750 Ki = 0.1413 nM 9.85
CHEMBL3298749 Ki = 0.3715 nM 9.43
CHEMBL220221 Ki = 0.3981 nM 9.40
CHEMBL3298745 Ki = 0.5754 nM 9.24
CHEMBL3298023 Ki = 0.7586 nM 9.12
CHEMBL3298746 Ki = 0.912 nM 9.04
CHEMBL3298017 Ki = 1.0 nM 9.00
CHEMBL3298748 Ki = 1.175 nM 8.93
CHEMBL220781 Ki = 1.259 nM 8.90
CHEMBL3298019 Ki = 1.66 nM 8.78
CHEMBL3298024 Ki = 2.291 nM 8.64
CHEMBL3298747 Ki = 3.236 nM 8.49
CHEMBL3298021 Ki = 3.311 nM 8.48
CHEMBL3298018 Ki = 4.074 nM 8.39
CHEMBL3298020 Ki = 5.012 nM 8.30
CHEMBL3298022 Ki = 5.495 nM 8.26