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Assay Detail

CHEMBL652741

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

Binding
Ability to displace [3H]-prazosin binding to rat cortical membranes expressing Alpha-1 adrenergic receptors
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Rowley M, Hallett DJ, Goodacre S, Moyes C, Crawforth J, Sparey TJ, Patel S, Marwood R, Patel S, Thomas S, Hitzel L, O'Connor D, Szeto N, Castro JL, Hutson PH, MacLeod AM.
J Med Chem (2001) 44 : 1603 -1614
PubMed 11334570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.78 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296512 1 8.96
CHEMBL496860 1 8.68
CHEMBL497054 1 8.55
CHEMBL523245 1 8.54
CHEMBL2368734 1 8.44
CHEMBL504699 1 8.42
CHEMBL497064 1 8.41
CHEMBL523585 1 8.17
CHEMBL507727 1 8.14
CHEMBL523760 1 8.14
CHEMBL496687 1 8.07
CHEMBL498048 1 7.80
CHEMBL507898 1 7.68
CHEMBL42557 1 7.68
CHEMBL497877 1 7.60
CHEMBL40584 1 7.60
CHEMBL498729 1 7.57
CHEMBL43819 1 7.52
CHEMBL496852 1 7.40
CHEMBL46523 1 7.33
CHEMBL43697 1 7.00
CHEMBL497878 1 6.68
CHEMBL2113667 1 6.60
CHEMBL295559 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296512 Ki = 1.1 nM 8.96
CHEMBL496860 Ki = 2.1 nM 8.68
CHEMBL497054 Ki = 2.8 nM 8.55
CHEMBL523245 Ki = 2.9 nM 8.54
CHEMBL2368734 Ki = 3.6 nM 8.44
CHEMBL504699 Ki = 3.8 nM 8.42
CHEMBL497064 Ki = 3.9 nM 8.41
CHEMBL523585 Ki = 6.7 nM 8.17
CHEMBL507727 Ki = 7.3 nM 8.14
CHEMBL523760 Ki = 7.3 nM 8.14
CHEMBL496687 Ki = 8.5 nM 8.07
CHEMBL498048 Ki = 16.0 nM 7.80
CHEMBL507898 Ki = 21.0 nM 7.68
CHEMBL42557 Ki = 21.0 nM 7.68
CHEMBL497877 Ki = 25.0 nM 7.60
CHEMBL40584 Ki = 25.0 nM 7.60
CHEMBL498729 Ki = 27.0 nM 7.57
CHEMBL43819 Ki = 30.0 nM 7.52
CHEMBL496852 Ki = 40.0 nM 7.40
CHEMBL46523 Ki = 47.0 nM 7.33
CHEMBL43697 Ki = 99.0 nM 7.00
CHEMBL497878 Ki = 210.0 nM 6.68
CHEMBL2113667 Ki = 250.0 nM 6.60
CHEMBL295559 Ki = 2100.0 nM 5.68