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Assay Detail

CHEMBL4179166

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

Binding
Displacement of [3H]-8-OH-DPAT from serotonin 5-HT1A receptor in Sprague-Dawley rat brain cortex homogenates incubated for 30 mins by liquid scintillation spectrometry
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New 5-HT1A, 5HT2A and 5HT2C receptor ligands containing a picolinic nucleus: Synthesis, in vitro and in vivo pharmacological evaluation.
Fiorino F, Magli E, Kędzierska E, Ciano A, Corvino A, Severino B, Perissutti E, Frecentese F, Di Vaio P, Saccone I, Izzo AA, Capasso R, Massarelli P, Rossi I, Orzelska-Gòrka J, Kotlińska JH, Santagada V, Caliendo G.
Bioorg Med Chem (2017) 25 : 5820 -5837
PubMed 28943244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 7.22 10.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209954 1 10.34
CHEMBL4208744 1 9.74
CHEMBL3763633 1 9.46
CHEMBL1202240 1 9.10
CHEMBL4202926 1 7.75
CHEMBL4214290 1 7.68
CHEMBL4207997 1 7.49
CHEMBL4211631 1 7.40
CHEMBL4208886 1 7.36
CHEMBL4210997 1 7.28
CHEMBL4212565 1 7.26
CHEMBL4210207 1 7.22
CHEMBL4205121 1 7.17
CHEMBL4215136 1 7.14
CHEMBL4217522 1 7.13
CHEMBL4204911 1 7.09
CHEMBL4203722 1 7.07
CHEMBL4214595 1 7.05
CHEMBL4218931 1 6.98
CHEMBL4218943 1 6.97
CHEMBL4205281 1 6.86
CHEMBL4217302 1 6.80
CHEMBL4217285 1 6.79
CHEMBL4206367 1 6.74
CHEMBL4214059 1 6.67
CHEMBL4218351 1 6.64
CHEMBL4209660 1 6.57
CHEMBL4204796 1 6.38
CHEMBL4206107 1 6.35
CHEMBL4205257 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209954 Ki = 0.046 nM 10.34
CHEMBL4208744 Ki = 0.183 nM 9.74
CHEMBL3763633 Ki = 0.344 nM 9.46
CHEMBL1202240 Ki = 0.8 nM 9.10
CHEMBL4202926 Ki = 17.9 nM 7.75
CHEMBL4214290 Ki = 20.8 nM 7.68
CHEMBL4207997 Ki = 32.7 nM 7.49
CHEMBL4211631 Ki = 40.1 nM 7.40
CHEMBL4208886 Ki = 44.1 nM 7.36
CHEMBL4210997 Ki = 52.7 nM 7.28
CHEMBL4212565 Ki = 55.4 nM 7.26
CHEMBL4210207 Ki = 59.5 nM 7.22
CHEMBL4205121 Ki = 68.0 nM 7.17
CHEMBL4215136 Ki = 71.6 nM 7.14
CHEMBL4217522 Ki = 74.8 nM 7.13
CHEMBL4204911 Ki = 82.0 nM 7.09
CHEMBL4203722 Ki = 85.6 nM 7.07
CHEMBL4214595 Ki = 88.7 nM 7.05
CHEMBL4218931 Ki = 104.0 nM 6.98
CHEMBL4218943 Ki = 108.0 nM 6.97
CHEMBL4205281 Ki = 138.0 nM 6.86
CHEMBL4217302 Ki = 158.0 nM 6.80
CHEMBL4217285 Ki = 161.0 nM 6.79
CHEMBL4206367 Ki = 181.0 nM 6.74
CHEMBL4214059 Ki = 215.0 nM 6.67
CHEMBL4218351 Ki = 230.0 nM 6.64
CHEMBL4209660 Ki = 267.0 nM 6.57
CHEMBL4204796 Ki = 412.0 nM 6.38
CHEMBL4206107 Ki = 443.0 nM 6.35
CHEMBL4205257 Ki = 495.0 nM 6.30
CHEMBL4218142 Ki = 500.0 nM 6.30
CHEMBL4204620 Ki = 540.0 nM 6.27
CHEMBL4205290 Ki = 599.0 nM 6.22
CHEMBL4209138 Ki = 1320.0 nM 5.88
CHEMBL4207703 Ki > 10000.0 nM -
CHEMBL4210519 Ki > 10000.0 nM -
CHEMBL4218771 Ki > 10000.0 nM -
CHEMBL4206623 Ki > 10000.0 nM -
CHEMBL4210471 Ki > 10000.0 nM -
CHEMBL4214076 Ki > 10000.0 nM -
CHEMBL4206752 Ki > 10000.0 nM -