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Assay Detail

CHEMBL3767882

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex incubated for 15 mins by liquid scintillation counting analysis
ChEMBL ↗
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 2A (CHEMBL322) ↗
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 7.49 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763812 — — 1 10.90
CHEMBL3763474 — — 1 10.41
CHEMBL3765231 — — 1 10.34
CHEMBL3764420 — — 1 9.64
CHEMBL3765470 — — 1 9.60
CHEMBL3764080 — — 1 9.10
CHEMBL51 KETANSERIN 3.0 1 9.07
CHEMBL3763558 — — 1 8.97
CHEMBL3764341 — — 1 8.45
CHEMBL3764761 — — 1 8.16
CHEMBL3765122 — — 1 8.01
CHEMBL3765463 — — 1 7.79
CHEMBL3764539 — — 1 7.45
CHEMBL3764752 — — 1 7.38
CHEMBL3764074 — — 1 7.26
CHEMBL3763242 — — 1 7.15
CHEMBL3764284 — — 1 7.03
CHEMBL3764666 — — 1 6.95
CHEMBL3764925 — — 1 6.74
CHEMBL3763834 — — 1 6.70
CHEMBL3764534 — — 1 6.68
CHEMBL3763714 — — 1 6.33
CHEMBL104593 — — 1 6.23
CHEMBL3764772 — — 1 6.20
CHEMBL3763633 — — 1 6.18
CHEMBL3764575 — — 1 6.11
CHEMBL3763429 — — 1 6.10
CHEMBL192242 — — 1 6.04
CHEMBL3764009 — — 1 5.90
CHEMBL3765273 — — 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763812 — Ki = 0.0126 nM 10.90
CHEMBL3763474 — Ki = 0.039 nM 10.41
CHEMBL3765231 — Ki = 0.046 nM 10.34
CHEMBL3764420 — Ki = 0.228 nM 9.64
CHEMBL3765470 — Ki = 0.254 nM 9.60
CHEMBL3764080 — Ki = 0.793 nM 9.10
CHEMBL51 KETANSERIN Ki = 0.85 nM 9.07
CHEMBL3763558 — Ki = 1.07 nM 8.97
CHEMBL3764341 — Ki = 3.53 nM 8.45
CHEMBL3764761 — Ki = 6.9 nM 8.16
CHEMBL3765122 — Ki = 9.85 nM 8.01
CHEMBL3765463 — Ki = 16.2 nM 7.79
CHEMBL3764539 — Ki = 35.5 nM 7.45
CHEMBL3764752 — Ki = 41.8 nM 7.38
CHEMBL3764074 — Ki = 54.6 nM 7.26
CHEMBL3763242 — Ki = 70.7 nM 7.15
CHEMBL3764284 — Ki = 92.6 nM 7.03
CHEMBL3764666 — Ki = 112.0 nM 6.95
CHEMBL3764925 — Ki = 182.0 nM 6.74
CHEMBL3763834 — Ki = 199.0 nM 6.70
CHEMBL3764534 — Ki = 207.0 nM 6.68
CHEMBL3763714 — Ki = 469.0 nM 6.33
CHEMBL104593 — Ki = 587.0 nM 6.23
CHEMBL3764772 — Ki = 631.0 nM 6.20
CHEMBL3763633 — Ki = 664.0 nM 6.18
CHEMBL3764575 — Ki = 770.0 nM 6.11
CHEMBL3763429 — Ki = 792.0 nM 6.10
CHEMBL192242 — Ki = 911.0 nM 6.04
CHEMBL3764009 — Ki = 1260.0 nM 5.90
CHEMBL3765273 — Ki = 1380.0 nM 5.86
CHEMBL3765622 — Ki = 2770.0 nM 5.56
CHEMBL3764313 — Ki = 3660.0 nM 5.44
CHEMBL3765808 — Ki > 10000.0 nM -
CHEMBL3765362 — Ki > 10000.0 nM -
CHEMBL3765471 — Ki = 0.00956 nM -
CHEMBL3764177 — Ki = 0.00985 nM -
CHEMBL3764390 — Ki > 10000.0 nM -
CHEMBL3765797 — Ki > 10000.0 nM -
CHEMBL3763629 — Ki > 10000.0 nM -
CHEMBL3763331 — Ki > 10000.0 nM -
CHEMBL3765643 — Ki > 10000.0 nM -