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Assay Detail

CHEMBL648047

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

Binding
In vitro binding affinity against rat cortical homogenate Alpha-1 adrenergic receptor using [3H]-prazosin as radioligand
ChEMBL ↗
54
Total Activities
54
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

New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
Mewshaw RE, Kavanagh J, Stack G, Marquis KL, Shi X, Kagan MZ, Webb MB, Katz AH, Park A, Kang YH, Abou-Gharbia M, Scerni R, Wasik T, Cortes-Burgos L, Spangler T, Brennan JA, Piesla M, Mazandarani H, Cockett MI, Ochalski R, Coupet J, Andree TH.
J Med Chem (1997) 40 : 4235 -4256
PubMed 9435894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 6.93 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136635 — — 1 8.52
CHEMBL134707 — — 1 8.22
CHEMBL134448 — — 1 8.05
CHEMBL134605 — — 1 8.02
CHEMBL134489 — — 1 8.02
CHEMBL134678 — — 1 7.96
CHEMBL135183 — — 1 7.89
CHEMBL134677 — — 1 7.89
CHEMBL135752 — — 1 7.77
CHEMBL134281 — — 1 7.75
CHEMBL135201 — — 1 7.75
CHEMBL424087 — — 1 7.60
CHEMBL334616 — — 1 7.55
CHEMBL133833 — — 1 7.46
CHEMBL134725 — — 1 7.46
CHEMBL135242 — — 1 7.44
CHEMBL543426 — — 1 7.42
CHEMBL423335 — — 1 7.42
CHEMBL134663 — — 1 7.40
CHEMBL134930 — — 1 7.38
CHEMBL135546 — — 1 7.37
CHEMBL135495 — — 1 7.20
CHEMBL337228 — — 1 7.16
CHEMBL135725 — — 1 7.01
CHEMBL135222 — — 1 6.96
CHEMBL135044 — — 1 6.92
CHEMBL135864 — — 1 6.84
CHEMBL134808 — — 1 6.80
CHEMBL340267 — — 1 6.80
CHEMBL135116 — — 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136635 — Ki = 3.0 nM 8.52
CHEMBL134707 — Ki = 6.0 nM 8.22
CHEMBL134448 — Ki = 9.0 nM 8.05
CHEMBL134605 — Ki = 9.5 nM 8.02
CHEMBL134489 — Ki = 9.5 nM 8.02
CHEMBL134678 — Ki = 11.0 nM 7.96
CHEMBL135183 — Ki = 13.0 nM 7.89
CHEMBL134677 — Ki = 13.0 nM 7.89
CHEMBL135752 — Ki = 17.0 nM 7.77
CHEMBL134281 — Ki = 18.0 nM 7.75
CHEMBL135201 — Ki = 18.0 nM 7.75
CHEMBL424087 — Ki = 25.0 nM 7.60
CHEMBL334616 — Ki = 28.0 nM 7.55
CHEMBL134725 — Ki = 35.0 nM 7.46
CHEMBL133833 — Ki = 35.0 nM 7.46
CHEMBL135242 — Ki = 36.0 nM 7.44
CHEMBL543426 — Ki = 38.0 nM 7.42
CHEMBL423335 — Ki = 38.0 nM 7.42
CHEMBL134663 — Ki = 40.0 nM 7.40
CHEMBL134930 — Ki = 42.0 nM 7.38
CHEMBL135546 — Ki = 43.0 nM 7.37
CHEMBL135495 — Ki = 63.5 nM 7.20
CHEMBL337228 — Ki = 69.0 nM 7.16
CHEMBL135725 — Ki = 98.0 nM 7.01
CHEMBL135222 — Ki = 111.0 nM 6.96
CHEMBL135044 — Ki = 120.0 nM 6.92
CHEMBL135864 — Ki = 145.0 nM 6.84
CHEMBL134808 — Ki = 160.0 nM 6.80
CHEMBL340267 — Ki = 160.0 nM 6.80
CHEMBL135116 — Ki = 177.0 nM 6.75
CHEMBL134807 — Ki = 212.0 nM 6.67
CHEMBL423890 — Ki = 254.0 nM 6.59
CHEMBL134343 — Ki = 285.0 nM 6.54
CHEMBL336856 — Ki = 307.0 nM 6.51
CHEMBL134655 — Ki = 315.0 nM 6.50
CHEMBL134843 — Ki = 375.0 nM 6.43
CHEMBL135137 — Ki = 414.0 nM 6.38
CHEMBL135269 — Ki = 452.0 nM 6.34
CHEMBL135357 — Ki = 487.0 nM 6.31
CHEMBL135297 — Ki = 500.0 nM 6.30
CHEMBL339190 — Ki = 504.0 nM 6.30
CHEMBL337724 — Ki = 514.0 nM 6.29
CHEMBL133367 — Ki = 579.0 nM 6.24
CHEMBL135395 — Ki = 572.5 nM 6.24
CHEMBL135636 — Ki = 582.0 nM 6.24
CHEMBL135873 — Ki = 624.0 nM 6.21
CHEMBL135211 — Ki = 641.0 nM 6.19
CHEMBL135291 — Ki = 811.0 nM 6.09
CHEMBL135285 — Ki = 1002.0 nM 6.00
CHEMBL337696 — Ki = 1136.0 nM 5.95