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Assay Detail

CHEMBL649437

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

Binding
Binding affinity for displacement of [3H]prazosin to rat Alpha-1 adrenergic receptor stably expressed in rat cortical membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.
J Med Chem (2002) 45 : 492 -503
PubMed 11784153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.78 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504699 1 8.40
CHEMBL357807 1 8.10
CHEMBL83894 FANANSERIN 2.0 1 7.89
CHEMBL343411 1 6.96
CHEMBL122761 1 6.80
CHEMBL149423 1 6.68
CHEMBL147431 1 6.62
CHEMBL150210 1 6.60
CHEMBL148418 1 6.60
CHEMBL148348 1 6.48
CHEMBL74355 VOLINANSERIN 3.0 1 6.38
CHEMBL147164 1 6.37
CHEMBL149510 1 6.34
CHEMBL149429 1 6.26
CHEMBL146233 1 6.18
CHEMBL146144 1 5.89
CHEMBL146485 1 -
CHEMBL146998 1 -
CHEMBL148280 1 -
CHEMBL146620 1 -
CHEMBL148565 1 -
CHEMBL146595 1 -
CHEMBL358075 1 -
CHEMBL147048 1 -
CHEMBL148058 1 -
CHEMBL145939 1 -
CHEMBL150220 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504699 Ki = 4.0 nM 8.40
CHEMBL357807 Ki = 8.0 nM 8.10
CHEMBL83894 FANANSERIN Ki = 13.0 nM 7.89
CHEMBL343411 Ki = 110.0 nM 6.96
CHEMBL122761 Ki = 160.0 nM 6.80
CHEMBL149423 Ki = 210.0 nM 6.68
CHEMBL147431 Ki = 240.0 nM 6.62
CHEMBL150210 Ki = 250.0 nM 6.60
CHEMBL148418 Ki = 250.0 nM 6.60
CHEMBL148348 Ki = 330.0 nM 6.48
CHEMBL74355 VOLINANSERIN Ki = 420.0 nM 6.38
CHEMBL147164 Ki = 430.0 nM 6.37
CHEMBL149510 Ki = 460.0 nM 6.34
CHEMBL149429 Ki = 550.0 nM 6.26
CHEMBL146233 Ki = 660.0 nM 6.18
CHEMBL146144 Ki = 1300.0 nM 5.89
CHEMBL146485 Ki > 1500.0 nM -
CHEMBL146998 Ki > 1500.0 nM -
CHEMBL148280 Ki > 1500.0 nM -
CHEMBL146620 Ki > 1500.0 nM -
CHEMBL148565 Ki > 1500.0 nM -
CHEMBL146595 Ki > 1500.0 nM -
CHEMBL358075 Ki > 1500.0 nM -
CHEMBL147048 Ki > 1500.0 nM -
CHEMBL148058 Ki > 1500.0 nM -
CHEMBL145939 Ki > 1500.0 nM -
CHEMBL150220 Ki > 1500.0 nM -