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Assay Detail

CHEMBL615772

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

Binding
Binding affinity to human 5-hydroxytryptamine 1A receptor was measured using [3H]-8-hydroxy-2-(di-n-propylamine) tetraline [3H]8-OH-DPAT) as radioligand
ChEMBL ↗
81
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 81 7.49 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298595 — — 1 9.47
CHEMBL60583 — — 1 9.27
CHEMBL13647 BMY-7378 — 1 9.10
CHEMBL299454 — — 1 8.97
CHEMBL57364 — — 1 8.96
CHEMBL56804 — — 1 8.92
CHEMBL56869 — — 1 8.89
CHEMBL59315 — — 1 8.87
CHEMBL57859 — — 1 8.63
CHEMBL57999 — — 1 8.47
CHEMBL56 8-OH-DPAT — 1 8.42
CHEMBL57540 — — 1 8.42
CHEMBL56878 — — 1 8.39
CHEMBL57593 — — 1 8.37
CHEMBL56292 — — 1 8.28
CHEMBL299022 — — 1 8.27
CHEMBL57747 — — 1 8.09
CHEMBL299253 — — 1 8.03
CHEMBL55647 — — 1 7.95
CHEMBL293980 — — 1 7.92
CHEMBL293539 — — 1 7.92
CHEMBL301019 — — 1 7.87
CHEMBL301224 — — 1 7.76
CHEMBL431943 — — 1 7.70
CHEMBL56150 — — 1 7.70
CHEMBL291908 — — 1 7.60
CHEMBL292686 — — 1 7.59
CHEMBL56805 — — 1 7.58
CHEMBL59262 — — 1 7.58
CHEMBL57868 — — 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298595 — Ki = 0.34 nM 9.47
CHEMBL60583 — Ki = 0.54 nM 9.27
CHEMBL13647 BMY-7378 Ki = 0.8 nM 9.10
CHEMBL299454 — Ki = 1.06 nM 8.97
CHEMBL57364 — Ki = 1.09 nM 8.96
CHEMBL56804 — Ki = 1.2 nM 8.92
CHEMBL56869 — Ki = 1.29 nM 8.89
CHEMBL59315 — Ki = 1.36 nM 8.87
CHEMBL57859 — Ki = 2.33 nM 8.63
CHEMBL57999 — Ki = 3.37 nM 8.47
CHEMBL56 8-OH-DPAT Ki = 3.8 nM 8.42
CHEMBL57540 — Ki = 3.84 nM 8.42
CHEMBL56878 — Ki = 4.07 nM 8.39
CHEMBL57593 — Ki = 4.24 nM 8.37
CHEMBL56292 — Ki = 5.25 nM 8.28
CHEMBL299022 — Ki = 5.37 nM 8.27
CHEMBL57747 — Ki = 8.22 nM 8.09
CHEMBL299253 — Ki = 9.38 nM 8.03
CHEMBL55647 — Ki = 11.27 nM 7.95
CHEMBL293980 — Ki = 12.08 nM 7.92
CHEMBL293539 — Ki = 12.07 nM 7.92
CHEMBL301019 — Ki = 13.44 nM 7.87
CHEMBL301224 — Ki = 17.43 nM 7.76
CHEMBL431943 — Ki = 19.97 nM 7.70
CHEMBL56150 — Ki = 19.82 nM 7.70
CHEMBL291908 — Ki = 25.35 nM 7.60
CHEMBL292686 — Ki = 25.9 nM 7.59
CHEMBL56805 — Ki = 26.27 nM 7.58
CHEMBL59262 — Ki = 26.15 nM 7.58
CHEMBL57868 — Ki = 29.64 nM 7.53
CHEMBL299691 — Ki = 32.57 nM 7.49
CHEMBL293968 — Ki = 35.71 nM 7.45
CHEMBL56438 — Ki = 36.0 nM 7.44
CHEMBL58476 — Ki = 52.31 nM 7.28
CHEMBL57168 — Ki = 54.59 nM 7.26
CHEMBL56899 — Ki = 62.22 nM 7.21
CHEMBL556313 — Ki = 61.0 nM 7.21
CHEMBL56403 — Ki = 65.8 nM 7.18
CHEMBL59149 — Ki = 69.55 nM 7.16
CHEMBL293734 — Ki = 85.4 nM 7.07
CHEMBL294829 — Ki = 86.25 nM 7.06
CHEMBL292366 — Ki = 91.86 nM 7.04
CHEMBL57317 — Ki = 104.1 nM 6.98
CHEMBL58930 — Ki = 125.3 nM 6.90
CHEMBL293111 — Ki = 127.84 nM 6.89
CHEMBL55654 — Ki = 134.84 nM 6.87
CHEMBL57546 — Ki = 153.0 nM 6.82
CHEMBL57882 — Ki = 160.3 nM 6.79
CHEMBL300152 — Ki = 206.96 nM 6.68
CHEMBL56851 — Ki = 234.4 nM 6.63