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Assay Detail

CHEMBL616791

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

Binding
Binding affinity at 5-hydroxytryptamine 1B receptor
34
Total Activities
34
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 1B (CHEMBL3459)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Characterization of potent and selective antagonists at postsynaptic 5-HT1A receptors in a series of N4-substituted arylpiperazines.
Peglion JL, Canton H, Bervoets K, Audinot V, Brocco M, Gobert A, Le Marouille-Girardon S, Millan MJ.
J Med Chem (1995) 38 : 4044 -4055
PubMed 7562940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.25 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282614 ELTOPRAZINE 2.0 1 7.27
CHEMBL131011 1 6.70
CHEMBL130734 1 6.69
CHEMBL131198 1 6.67
CHEMBL131200 1 6.64
CHEMBL130870 1 6.60
CHEMBL129947 1 6.50
CHEMBL131018 1 6.50
CHEMBL128546 1 6.42
CHEMBL341391 1 6.38
CHEMBL335010 1 6.31
CHEMBL334381 1 6.26
CHEMBL131184 1 6.25
CHEMBL130276 1 6.22
CHEMBL337078 1 6.21
CHEMBL131900 1 6.20
CHEMBL130976 1 6.19
CHEMBL133188 1 6.17
CHEMBL129993 1 6.16
CHEMBL341390 1 6.15
CHEMBL132514 1 6.15
CHEMBL337279 1 6.11
CHEMBL335297 1 6.10
CHEMBL131324 1 6.04
CHEMBL337036 1 6.03
CHEMBL8618 NAN-190 1 5.97
CHEMBL132657 1 5.96
CHEMBL335752 1 5.85
CHEMBL127216 1 5.85
CHEMBL132878 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282614 ELTOPRAZINE Ki = 53.7 nM 7.27
CHEMBL131011 Ki = 199.53 nM 6.70
CHEMBL130734 Ki = 204.17 nM 6.69
CHEMBL131198 Ki = 213.8 nM 6.67
CHEMBL131200 Ki = 229.09 nM 6.64
CHEMBL130870 Ki = 251.19 nM 6.60
CHEMBL129947 Ki = 316.23 nM 6.50
CHEMBL131018 Ki = 316.23 nM 6.50
CHEMBL128546 Ki = 380.19 nM 6.42
CHEMBL341391 Ki = 416.87 nM 6.38
CHEMBL335010 Ki = 489.78 nM 6.31
CHEMBL334381 Ki = 549.54 nM 6.26
CHEMBL131184 Ki = 562.34 nM 6.25
CHEMBL130276 Ki = 602.56 nM 6.22
CHEMBL337078 Ki = 616.6 nM 6.21
CHEMBL131900 Ki = 630.96 nM 6.20
CHEMBL130976 Ki = 645.65 nM 6.19
CHEMBL133188 Ki = 676.08 nM 6.17
CHEMBL129993 Ki = 691.83 nM 6.16
CHEMBL341390 Ki = 707.95 nM 6.15
CHEMBL132514 Ki = 707.95 nM 6.15
CHEMBL337279 Ki = 776.25 nM 6.11
CHEMBL335297 Ki = 794.33 nM 6.10
CHEMBL131324 Ki = 912.01 nM 6.04
CHEMBL337036 Ki = 933.25 nM 6.03
CHEMBL8618 NAN-190 Ki = 1071.52 nM 5.97
CHEMBL132657 Ki = 1096.48 nM 5.96
CHEMBL335752 Ki = 1412.54 nM 5.85
CHEMBL127216 Ki = 1412.54 nM 5.85
CHEMBL132878 Ki = 1513.56 nM 5.82
CHEMBL49247 Ki = 1778.28 nM 5.75
CHEMBL130103 Ki = 1862.09 nM 5.73
CHEMBL13647 BMY-7378 Ki > 10000.0 nM -
CHEMBL38288 Ki > 10000.0 nM -