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Assay Detail

CHEMBL617560

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Binding
Binding affinity for 5-hydroxytryptamine 1D receptor
ChEMBL ↗
47
Total Activities
47
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 1D (CHEMBL4105) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

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 47 5.11 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27403 — — 1 6.91
CHEMBL64948 — — 1 6.87
CHEMBL62274 — — 1 6.42
CHEMBL65974 — — 1 6.40
CHEMBL51118 — — 1 6.33
CHEMBL301765 — — 1 6.22
CHEMBL302225 — — 1 6.04
CHEMBL68390 — — 1 5.90
CHEMBL65736 — — 1 5.59
CHEMBL294368 — — 1 5.51
CHEMBL18772 QUIPAZINE 2.0 1 5.43
CHEMBL54720 — — 1 4.85
CHEMBL292725 — — 1 4.70
CHEMBL64727 — — 1 4.60
CHEMBL302447 — — 1 4.51
CHEMBL62445 — — 1 4.45
CHEMBL62902 — — 1 4.45
CHEMBL63790 — — 1 4.44
CHEMBL64903 — — 1 4.42
CHEMBL302431 — — 1 4.35
CHEMBL63845 — — 1 4.24
CHEMBL65669 — — 1 4.22
CHEMBL62366 — — 1 4.06
CHEMBL65710 — — 1 4.03
CHEMBL292293 — — 1 4.03
CHEMBL293879 — — 1 4.00
CHEMBL418678 — — 1 -
CHEMBL66310 — — 1 -
CHEMBL63905 — — 1 -
CHEMBL66540 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27403 — IC50 = 123.03 nM 6.91
CHEMBL64948 — IC50 = 134.9 nM 6.87
CHEMBL62274 — IC50 = 380.19 nM 6.42
CHEMBL65974 — IC50 = 398.11 nM 6.40
CHEMBL51118 — IC50 = 467.74 nM 6.33
CHEMBL301765 — IC50 = 602.56 nM 6.22
CHEMBL302225 — IC50 = 912.01 nM 6.04
CHEMBL68390 — IC50 = 1258.93 nM 5.90
CHEMBL65736 — IC50 = 2570.4 nM 5.59
CHEMBL294368 — IC50 = 3090.3 nM 5.51
CHEMBL18772 QUIPAZINE IC50 = 3715.35 nM 5.43
CHEMBL54720 — IC50 = 14125.38 nM 4.85
CHEMBL292725 — IC50 = 19952.62 nM 4.70
CHEMBL64727 — IC50 = 25118.86 nM 4.60
CHEMBL302447 — IC50 = 30902.95 nM 4.51
CHEMBL62445 — IC50 = 35481.34 nM 4.45
CHEMBL62902 — IC50 = 35481.34 nM 4.45
CHEMBL63790 — IC50 = 36307.81 nM 4.44
CHEMBL64903 — IC50 = 38018.94 nM 4.42
CHEMBL302431 — IC50 = 44668.36 nM 4.35
CHEMBL63845 — IC50 = 57543.99 nM 4.24
CHEMBL65669 — IC50 = 60255.96 nM 4.22
CHEMBL62366 — IC50 = 87096.36 nM 4.06
CHEMBL65710 — IC50 = 93325.43 nM 4.03
CHEMBL292293 — IC50 = 93325.43 nM 4.03
CHEMBL293879 — IC50 = 100000.0 nM 4.00
CHEMBL66307 — IC50 > 100000.0 nM -
CHEMBL302104 — IC50 > 100000.0 nM -
CHEMBL293219 — IC50 > 100000.0 nM -
CHEMBL417570 — IC50 = 128824.96 nM -
CHEMBL63289 — IC50 = 512861.38 nM -
CHEMBL62612 — IC50 = 524807.46 nM -
CHEMBL62911 — IC50 > 100000.0 nM -
CHEMBL63588 — IC50 > 100000.0 nM -
CHEMBL65212 — IC50 > 100000.0 nM -
CHEMBL66408 — IC50 = 537031.8 nM -
CHEMBL52772 — IC50 > 100000.0 nM -
CHEMBL261977 — IC50 = 104712.85 nM -
CHEMBL303986 — IC50 = 251188.64 nM -
CHEMBL63114 — IC50 > 100000.0 nM -
CHEMBL63713 — IC50 = 199526.23 nM -
CHEMBL64559 — IC50 > 100000.0 nM -
CHEMBL65413 — IC50 = 257039.58 nM -
CHEMBL66540 — IC50 > 100000.0 nM -
CHEMBL63905 — IC50 = 275422.87 nM -
CHEMBL66310 — IC50 > 100000.0 nM -
CHEMBL418678 — IC50 = 138038.43 nM -