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Assay Detail

CHEMBL873475

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

Binding
Binding affinity for 5-hydroxytryptamine 1B receptor
46
Total Activities
46
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1B (CHEMBL3459)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
Rault S, Lancelot JC, Prunier H, Robba M, Renard P, Delagrange P, Pfeiffer B, Caignard DH, Guardiola-Lemaitre B, Hamon M.
J Med Chem (1996) 39 : 2068 -2080
PubMed 8642566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.28 7.86
-Log IC50 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301765 1 7.86
CHEMBL27403 1 6.47
CHEMBL51118 1 6.38
CHEMBL62274 1 6.24
CHEMBL261977 1 6.19
CHEMBL293879 1 6.17
CHEMBL54720 1 5.99
CHEMBL64948 1 5.96
CHEMBL63790 1 5.51
CHEMBL302431 1 5.37
CHEMBL294368 1 5.33
CHEMBL18772 QUIPAZINE 2.0 1 5.15
CHEMBL292725 1 5.15
CHEMBL63845 1 5.13
CHEMBL65736 1 4.99
CHEMBL65974 1 4.95
CHEMBL418678 1 4.84
CHEMBL62366 1 4.83
CHEMBL63713 1 4.73
CHEMBL62902 1 4.72
CHEMBL64903 1 4.71
CHEMBL302447 1 4.62
CHEMBL65413 1 4.47
CHEMBL62911 1 4.39
CHEMBL64727 1 4.20
CHEMBL63905 1 4.15
CHEMBL65710 1 4.04
CHEMBL66540 1 -
CHEMBL66310 1 -
CHEMBL64559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301765 IC50 = 13.8 nM 7.86
CHEMBL27403 IC50 = 338.84 nM 6.47
CHEMBL51118 IC50 = 416.87 nM 6.38
CHEMBL62274 IC50 = 575.44 nM 6.24
CHEMBL261977 IC50 = 645.65 nM 6.19
CHEMBL293879 IC50 = 676.08 nM 6.17
CHEMBL54720 IC50 = 1023.29 nM 5.99
CHEMBL64948 IC50 = 1096.48 nM 5.96
CHEMBL63790 IC50 = 3090.3 nM 5.51
CHEMBL302431 IC50 = 4265.8 nM 5.37
CHEMBL294368 IC50 = 4677.35 nM 5.33
CHEMBL18772 QUIPAZINE IC50 = 7079.46 nM 5.15
CHEMBL292725 IC50 = 7079.46 nM 5.15
CHEMBL63845 IC50 = 7413.1 nM 5.13
CHEMBL65736 IC50 = 10232.93 nM 4.99
CHEMBL65974 IC50 = 11220.18 nM 4.95
CHEMBL418678 IC50 = 14454.4 nM 4.84
CHEMBL62366 IC50 = 14791.08 nM 4.83
CHEMBL63713 IC50 = 18620.87 nM 4.73
CHEMBL62902 IC50 = 19054.61 nM 4.72
CHEMBL64903 IC50 = 19498.45 nM 4.71
CHEMBL302447 IC50 = 23988.33 nM 4.62
CHEMBL65413 IC50 = 33884.42 nM 4.47
CHEMBL62911 IC50 = 40738.03 nM 4.39
CHEMBL64727 IC50 = 63095.73 nM 4.20
CHEMBL63905 IC50 = 70794.58 nM 4.15
CHEMBL65710 IC50 = 91201.08 nM 4.04
CHEMBL62445 IC50 > 100000.0 nM -
CHEMBL66307 IC50 > 100000.0 nM -
CHEMBL65669 IC50 > 100000.0 nM -
CHEMBL302104 -Log IC50 - -
CHEMBL293219 IC50 = 1380384.26 nM -
CHEMBL417570 IC50 = 112201.85 nM -
CHEMBL68390 -Log IC50 - -
CHEMBL292293 IC50 > 100000.0 nM -
CHEMBL63289 -Log IC50 - -
CHEMBL62612 IC50 > 100000.0 nM -
CHEMBL63588 IC50 > 100000.0 nM -
CHEMBL66408 IC50 > 100000.0 nM -
CHEMBL52772 IC50 = 1584893.19 nM -
CHEMBL303986 IC50 > 100000.0 nM -
CHEMBL63114 IC50 > 100000.0 nM -
CHEMBL65212 -Log IC50 - -
CHEMBL64559 IC50 > 100000.0 nM -
CHEMBL66310 IC50 = 301995.17 nM -
CHEMBL66540 IC50 > 100000.0 nM -