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Assay Detail

CHEMBL3767883

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex incubated for 30 mins by liquid scintillation counting analysis
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

Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.
Fiorino F, Ciano A, Magli E, Severino B, Corvino A, Perissutti E, Frecentese F, Di Vaio P, Izzo AA, Capasso R, Massarelli P, Nencini C, Rossi I, Kędzierska E, Orzelska-Gòrka J, Bielenica A, Santagada V, Caliendo G.
Eur J Med Chem (2016) 110 : 133 -150
PubMed 26820556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 7.55 10.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764390 1 10.95
CHEMBL3763331 1 9.89
CHEMBL104593 1 9.44
CHEMBL3764761 1 9.18
CHEMBL505765 1 9.10
CHEMBL3764539 1 9.09
CHEMBL3765362 1 8.97
CHEMBL3763714 1 8.54
CHEMBL3765463 1 8.32
CHEMBL3764752 1 8.28
CHEMBL3764575 1 8.07
CHEMBL3763834 1 8.06
CHEMBL3764177 1 8.04
CHEMBL3764534 1 8.02
CHEMBL3765471 1 8.00
CHEMBL3763812 1 7.97
CHEMBL3765470 1 7.86
CHEMBL3764074 1 7.82
CHEMBL3763242 1 7.78
CHEMBL3764009 1 7.61
CHEMBL3764080 1 7.44
CHEMBL3764666 1 7.25
CHEMBL3764313 1 7.14
CHEMBL3763429 1 7.00
CHEMBL3764420 1 7.00
CHEMBL3764925 1 6.91
CHEMBL3764284 1 6.91
CHEMBL3765622 1 6.80
CHEMBL3763558 1 6.66
CHEMBL3764341 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764390 Ki = 0.0113 nM 10.95
CHEMBL3763331 Ki = 0.13 nM 9.89
CHEMBL104593 Ki = 0.36 nM 9.44
CHEMBL3764761 Ki = 0.658 nM 9.18
CHEMBL505765 Ki = 0.8 nM 9.10
CHEMBL3764539 Ki = 0.82 nM 9.09
CHEMBL3765362 Ki = 1.08 nM 8.97
CHEMBL3763714 Ki = 2.85 nM 8.54
CHEMBL3765463 Ki = 4.77 nM 8.32
CHEMBL3764752 Ki = 5.23 nM 8.28
CHEMBL3764575 Ki = 8.42 nM 8.07
CHEMBL3763834 Ki = 8.74 nM 8.06
CHEMBL3764177 Ki = 9.19 nM 8.04
CHEMBL3764534 Ki = 9.59 nM 8.02
CHEMBL3765471 Ki = 10.0 nM 8.00
CHEMBL3763812 Ki = 10.6 nM 7.97
CHEMBL3765470 Ki = 13.9 nM 7.86
CHEMBL3764074 Ki = 15.2 nM 7.82
CHEMBL3763242 Ki = 16.7 nM 7.78
CHEMBL3764009 Ki = 24.7 nM 7.61
CHEMBL3764080 Ki = 36.2 nM 7.44
CHEMBL3764666 Ki = 56.7 nM 7.25
CHEMBL3764313 Ki = 72.5 nM 7.14
CHEMBL3763429 Ki = 100.0 nM 7.00
CHEMBL3764420 Ki = 99.1 nM 7.00
CHEMBL3764925 Ki = 122.0 nM 6.91
CHEMBL3764284 Ki = 124.0 nM 6.91
CHEMBL3765622 Ki = 157.0 nM 6.80
CHEMBL3763558 Ki = 219.0 nM 6.66
CHEMBL3764341 Ki = 325.0 nM 6.49
CHEMBL3763633 Ki = 334.0 nM 6.48
CHEMBL3763474 Ki = 331.0 nM 6.48
CHEMBL3765122 Ki = 455.0 nM 6.34
CHEMBL3764772 Ki = 549.0 nM 6.26
CHEMBL3765231 Ki = 549.0 nM 6.26
CHEMBL3765273 Ki = 590.0 nM 6.23
CHEMBL3765797 Ki = 779.0 nM 6.11
CHEMBL3765643 Ki = 1060.0 nM 5.97
CHEMBL192242 Ki = 1270.0 nM 5.90
CHEMBL3765808 Ki = 3310.0 nM 5.48
CHEMBL3763629 Ki > 10000.0 nM -