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Assay Detail

CHEMBL646170

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

Binding
In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens.
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Alpha-1A adrenergic receptor (CHEMBL319) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.
Leonardi A, Barlocco D, Montesano F, Cignarella G, Motta G, Testa R, Poggesi E, Seeber M, De Benedetti PG, Fanelli F.
J Med Chem (2004) 47 : 1900 -1918
PubMed 15055991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 6.91 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59262 — — 1 8.74
CHEMBL56292 — — 1 8.70
CHEMBL55319 — — 1 8.54
CHEMBL60583 — — 1 8.45
CHEMBL56804 — — 1 7.96
CHEMBL292366 — — 1 7.57
CHEMBL57540 — — 1 7.53
CHEMBL301224 — — 1 7.37
CHEMBL55655 — — 1 7.36
CHEMBL299253 — — 1 7.27
CHEMBL57859 — — 1 7.26
CHEMBL57317 — — 1 7.22
CHEMBL56620 — — 1 7.17
CHEMBL294235 — — 1 7.11
CHEMBL299454 — — 1 7.06
CHEMBL294646 — — 1 7.04
CHEMBL293539 — — 1 6.97
CHEMBL56899 — — 1 6.94
CHEMBL55882 — — 1 6.92
CHEMBL431354 — — 1 6.92
CHEMBL440118 — — 1 6.92
CHEMBL59149 — — 1 6.90
CHEMBL56438 — — 1 6.89
CHEMBL556313 — — 1 6.87
CHEMBL300152 — — 1 6.73
CHEMBL55654 — — 1 6.72
CHEMBL299022 — — 1 6.67
CHEMBL60699 — — 1 6.53
CHEMBL298595 — — 1 6.53
CHEMBL293111 — — 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59262 — Ki = 1.81 nM 8.74
CHEMBL56292 — Ki = 2.01 nM 8.70
CHEMBL55319 — Ki = 2.85 nM 8.54
CHEMBL60583 — Ki = 3.54 nM 8.45
CHEMBL56804 — Ki = 10.89 nM 7.96
CHEMBL292366 — Ki = 27.21 nM 7.57
CHEMBL57540 — Ki = 29.25 nM 7.53
CHEMBL301224 — Ki = 42.41 nM 7.37
CHEMBL55655 — Ki = 43.96 nM 7.36
CHEMBL299253 — Ki = 53.93 nM 7.27
CHEMBL57859 — Ki = 54.43 nM 7.26
CHEMBL57317 — Ki = 59.82 nM 7.22
CHEMBL56620 — Ki = 68.26 nM 7.17
CHEMBL294235 — Ki = 77.88 nM 7.11
CHEMBL299454 — Ki = 87.55 nM 7.06
CHEMBL294646 — Ki = 91.96 nM 7.04
CHEMBL293539 — Ki = 107.7 nM 6.97
CHEMBL56899 — Ki = 114.06 nM 6.94
CHEMBL55882 — Ki = 119.6 nM 6.92
CHEMBL431354 — Ki = 119.28 nM 6.92
CHEMBL440118 — Ki = 118.74 nM 6.92
CHEMBL59149 — Ki = 125.55 nM 6.90
CHEMBL56438 — Ki = 128.0 nM 6.89
CHEMBL556313 — Ki = 135.12 nM 6.87
CHEMBL300152 — Ki = 186.68 nM 6.73
CHEMBL55654 — Ki = 190.25 nM 6.72
CHEMBL299022 — Ki = 213.6 nM 6.67
CHEMBL60699 — Ki = 294.4 nM 6.53
CHEMBL298595 — Ki = 295.1 nM 6.53
CHEMBL293111 — Ki = 330.51 nM 6.48
CHEMBL56869 — Ki = 376.41 nM 6.42
CHEMBL292399 — Ki = 414.1 nM 6.38
CHEMBL431943 — Ki = 421.6 nM 6.38
CHEMBL58384 — Ki = 479.5 nM 6.32
CHEMBL13647 BMY-7378 Ki = 494.7 nM 6.31
CHEMBL57868 — Ki = 503.2 nM 6.30
CHEMBL57593 — Ki = 551.61 nM 6.26
CHEMBL291908 — Ki = 584.16 nM 6.23
CHEMBL57098 — Ki = 630.84 nM 6.20
CHEMBL55790 — Ki = 786.3 nM 6.10
CHEMBL57097 — Ki = 1518.7 nM 5.82
CHEMBL56 8-OH-DPAT Ki = 2082.0 nM 5.68
CHEMBL293968 — Ki = 3355.0 nM 5.47
CHEMBL301019 — Ki > 1000.0 nM -
CHEMBL57882 — Ki > 1000.0 nM -
CHEMBL417939 — Ki > 1000.0 nM -
CHEMBL57364 — Ki > 1000.0 nM -
CHEMBL299691 — Ki > 1000.0 nM -
CHEMBL292686 — Ki > 1000.0 nM -
CHEMBL293734 — Ki > 1000.0 nM -