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Assay Detail

CHEMBL615580

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Binding
Binding affinity for 5-hydroxytryptamine 1A 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 1A (CHEMBL214) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.86 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27403 — — 1 7.33
CHEMBL302225 — — 1 7.28
CHEMBL301765 — — 1 7.23
CHEMBL65736 — — 1 7.21
CHEMBL51118 — — 1 7.17
CHEMBL63713 — — 1 7.14
CHEMBL261977 — — 1 7.08
CHEMBL64948 — — 1 7.03
CHEMBL65974 — — 1 6.93
CHEMBL62274 — — 1 6.92
CHEMBL293879 — — 1 6.59
CHEMBL63790 — — 1 6.58
CHEMBL68390 — — 1 6.54
CHEMBL418678 — — 1 6.46
CHEMBL54720 — — 1 6.40
CHEMBL303986 — — 1 6.39
CHEMBL294368 — — 1 6.18
CHEMBL292725 — — 1 5.98
CHEMBL302431 — — 1 5.87
CHEMBL18772 QUIPAZINE 2.0 1 5.84
CHEMBL62366 — — 1 5.31
CHEMBL65710 — — 1 5.23
CHEMBL62445 — — 1 5.21
CHEMBL62911 — — 1 5.11
CHEMBL64903 — — 1 5.11
CHEMBL65413 — — 1 4.99
CHEMBL63845 — — 1 4.90
CHEMBL52772 — — 1 4.84
CHEMBL65669 — — 1 4.81
CHEMBL62902 — — 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27403 — IC50 = 46.77 nM 7.33
CHEMBL302225 — IC50 = 52.48 nM 7.28
CHEMBL301765 — IC50 = 58.88 nM 7.23
CHEMBL65736 — IC50 = 61.66 nM 7.21
CHEMBL51118 — IC50 = 67.61 nM 7.17
CHEMBL63713 — IC50 = 72.44 nM 7.14
CHEMBL261977 — IC50 = 83.18 nM 7.08
CHEMBL64948 — IC50 = 93.33 nM 7.03
CHEMBL65974 — IC50 = 117.49 nM 6.93
CHEMBL62274 — IC50 = 120.23 nM 6.92
CHEMBL293879 — IC50 = 257.04 nM 6.59
CHEMBL63790 — IC50 = 263.03 nM 6.58
CHEMBL68390 — IC50 = 288.4 nM 6.54
CHEMBL418678 — IC50 = 346.74 nM 6.46
CHEMBL54720 — IC50 = 398.11 nM 6.40
CHEMBL303986 — IC50 = 407.38 nM 6.39
CHEMBL294368 — IC50 = 660.69 nM 6.18
CHEMBL292725 — IC50 = 1047.13 nM 5.98
CHEMBL302431 — IC50 = 1348.96 nM 5.87
CHEMBL18772 QUIPAZINE IC50 = 1445.44 nM 5.84
CHEMBL62366 — IC50 = 4897.79 nM 5.31
CHEMBL65710 — IC50 = 5888.44 nM 5.23
CHEMBL62445 — IC50 = 6165.95 nM 5.21
CHEMBL62911 — IC50 = 7762.47 nM 5.11
CHEMBL64903 — IC50 = 7762.47 nM 5.11
CHEMBL65413 — IC50 = 10232.93 nM 4.99
CHEMBL63845 — IC50 = 12589.25 nM 4.90
CHEMBL52772 — IC50 = 14454.4 nM 4.84
CHEMBL65669 — IC50 = 15488.17 nM 4.81
CHEMBL62902 — IC50 = 17782.79 nM 4.75
CHEMBL302447 — IC50 = 25703.96 nM 4.59
CHEMBL64727 — IC50 = 31622.78 nM 4.50
CHEMBL292293 — IC50 = 32359.37 nM 4.49
CHEMBL63289 — IC50 = 33884.42 nM 4.47
CHEMBL63905 — IC50 = 43651.58 nM 4.36
CHEMBL63114 — IC50 = 64565.42 nM 4.19
CHEMBL66307 — IC50 = 204173.79 nM -
CHEMBL64559 — IC50 > 100000.0 nM -
CHEMBL302104 — IC50 > 100000.0 nM -
CHEMBL66540 — IC50 > 100000.0 nM -
CHEMBL293219 — IC50 > 100000.0 nM -
CHEMBL417570 — IC50 = 102329.3 nM -
CHEMBL65212 — IC50 = 457088.19 nM -
CHEMBL66310 — IC50 > 100000.0 nM -
CHEMBL62612 — IC50 = 125892.54 nM -
CHEMBL63588 — IC50 > 100000.0 nM -
CHEMBL66408 — IC50 = 389045.14 nM -