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Assay Detail

CHEMBL649207

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

Binding
Binding affinity constant against alpha-1B adrenergic receptor of guinea pig spleen
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Spleen
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1B adrenergic receptor (CHEMBL232)
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 53 7.23 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60583 1 8.30
CHEMBL59262 1 8.27
CHEMBL556313 1 8.23
CHEMBL56292 1 8.11
CHEMBL301224 1 8.10
CHEMBL417939 1 8.09
CHEMBL56438 1 8.00
CHEMBL293539 1 8.00
CHEMBL298595 1 7.94
CHEMBL300152 1 7.88
CHEMBL55319 1 7.87
CHEMBL292366 1 7.80
CHEMBL57868 1 7.77
CHEMBL299253 1 7.69
CHEMBL55654 1 7.58
CHEMBL56804 1 7.45
CHEMBL299454 1 7.44
CHEMBL440118 1 7.42
CHEMBL57317 1 7.36
CHEMBL299022 1 7.34
CHEMBL56899 1 7.32
CHEMBL293111 1 7.28
CHEMBL294235 1 7.27
CHEMBL57859 1 7.26
CHEMBL431943 1 7.24
CHEMBL299691 1 7.20
CHEMBL291908 1 7.13
CHEMBL55882 1 7.10
CHEMBL56620 1 7.08
CHEMBL293734 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60583 Ki = 4.97 nM 8.30
CHEMBL59262 Ki = 5.38 nM 8.27
CHEMBL556313 Ki = 5.88 nM 8.23
CHEMBL56292 Ki = 7.76 nM 8.11
CHEMBL301224 Ki = 7.95 nM 8.10
CHEMBL417939 Ki = 8.21 nM 8.09
CHEMBL56438 Ki = 9.9 nM 8.00
CHEMBL293539 Ki = 10.05 nM 8.00
CHEMBL298595 Ki = 11.5 nM 7.94
CHEMBL300152 Ki = 13.11 nM 7.88
CHEMBL55319 Ki = 13.61 nM 7.87
CHEMBL292366 Ki = 15.84 nM 7.80
CHEMBL57868 Ki = 17.01 nM 7.77
CHEMBL299253 Ki = 20.25 nM 7.69
CHEMBL55654 Ki = 26.6 nM 7.58
CHEMBL56804 Ki = 35.56 nM 7.45
CHEMBL299454 Ki = 35.94 nM 7.44
CHEMBL440118 Ki = 37.57 nM 7.42
CHEMBL57317 Ki = 43.35 nM 7.36
CHEMBL299022 Ki = 46.18 nM 7.34
CHEMBL56899 Ki = 47.54 nM 7.32
CHEMBL293111 Ki = 52.89 nM 7.28
CHEMBL294235 Ki = 54.08 nM 7.27
CHEMBL57859 Ki = 54.99 nM 7.26
CHEMBL431943 Ki = 57.65 nM 7.24
CHEMBL299691 Ki = 62.62 nM 7.20
CHEMBL291908 Ki = 73.53 nM 7.13
CHEMBL55882 Ki = 79.62 nM 7.10
CHEMBL56620 Ki = 83.61 nM 7.08
CHEMBL293734 Ki = 84.08 nM 7.08
CHEMBL294646 Ki = 86.38 nM 7.06
CHEMBL57593 Ki = 86.96 nM 7.06
CHEMBL58476 Ki = 119.18 nM 6.92
CHEMBL56869 Ki = 122.03 nM 6.91
CHEMBL292399 Ki = 127.8 nM 6.89
CHEMBL57540 Ki = 131.95 nM 6.88
CHEMBL431354 Ki = 168.28 nM 6.77
CHEMBL13647 BMY-7378 Ki = 168.2 nM 6.77
CHEMBL59149 Ki = 193.29 nM 6.71
CHEMBL57364 Ki = 220.52 nM 6.66
CHEMBL60699 Ki = 262.76 nM 6.58
CHEMBL293968 Ki = 264.47 nM 6.58
CHEMBL292686 Ki = 274.38 nM 6.56
CHEMBL58384 Ki = 447.86 nM 6.35
CHEMBL294023 Ki = 790.88 nM 6.10
CHEMBL55655 Ki = 812.58 nM 6.09
CHEMBL55790 Ki = 915.4 nM 6.04
CHEMBL56 8-OH-DPAT Ki = 1882.0 nM 5.72
CHEMBL57098 Ki > 1000.0 nM -
CHEMBL301019 Ki > 1000.0 nM -