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Assay Detail

CHEMBL4199347

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

Binding
Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL ↗
42
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of β-Arrestin Biased Ligands of 5-HT7R.
Kim Y, Kim H, Lee J, Lee JK, Min SJ, Seong J, Rhim H, Tae J, Lee HJ, Choo H.
J Med Chem (2018) 61 : 7218 -7233
PubMed 30028132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 6.72 9.47
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282199 — — 2 9.47
CHEMBL4215875 — — 2 7.80
CHEMBL4207884 — — 2 7.52
CHEMBL4210782 — — 2 7.33
CHEMBL4218672 — — 2 7.28
CHEMBL4218801 — — 2 7.16
CHEMBL4209274 — — 2 6.98
CHEMBL4215925 — — 2 6.50
CHEMBL4213135 — — 2 6.49
CHEMBL4206411 — — 2 6.44
CHEMBL4207073 — — 2 6.43
CHEMBL4214171 — — 2 6.41
CHEMBL4213067 — — 2 6.37
CHEMBL4207901 — — 2 6.30
CHEMBL4205846 — — 2 6.15
CHEMBL4215197 — — 2 6.05
CHEMBL4202995 — — 2 6.05
CHEMBL4217548 — — 2 5.91
CHEMBL4211303 — — 2 5.85
CHEMBL4203526 — — 2 5.84
CHEMBL4202720 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282199 — Ki = 0.34 nM 9.47
CHEMBL282199 — Ki = 0.3388 nM 9.47
CHEMBL4215875 — Ki = 16.0 nM 7.80
CHEMBL4215875 — Ki = 16.22 nM 7.79
CHEMBL4207884 — Ki = 30.0 nM 7.52
CHEMBL4207884 — Ki = 31.62 nM 7.50
CHEMBL4210782 — Ki = 46.77 nM 7.33
CHEMBL4210782 — Ki = 47.0 nM 7.33
CHEMBL4218672 — Ki = 52.48 nM 7.28
CHEMBL4218672 — Ki = 53.0 nM 7.28
CHEMBL4218801 — Ki = 70.0 nM 7.16
CHEMBL4218801 — Ki = 70.79 nM 7.15
CHEMBL4209274 — Ki = 104.0 nM 6.98
CHEMBL4209274 — Ki = 104.71 nM 6.98
CHEMBL4215925 — Ki = 316.23 nM 6.50
CHEMBL4215925 — Ki = 319.0 nM 6.50
CHEMBL4213135 — Ki = 322.0 nM 6.49
CHEMBL4213135 — Ki = 323.59 nM 6.49
CHEMBL4206411 — Ki = 363.08 nM 6.44
CHEMBL4206411 — Ki = 366.0 nM 6.44
CHEMBL4207073 — Ki = 371.54 nM 6.43
CHEMBL4207073 — Ki = 369.0 nM 6.43
CHEMBL4214171 — Ki = 386.0 nM 6.41
CHEMBL4214171 — Ki = 389.05 nM 6.41
CHEMBL4213067 — Ki = 425.0 nM 6.37
CHEMBL4213067 — Ki = 426.58 nM 6.37
CHEMBL4207901 — Ki = 501.19 nM 6.30
CHEMBL4207901 — Ki = 506.0 nM 6.30
CHEMBL4205846 — Ki = 714.0 nM 6.15
CHEMBL4205846 — Ki = 707.95 nM 6.15
CHEMBL4215197 — Ki = 881.0 nM 6.05
CHEMBL4202995 — Ki = 883.0 nM 6.05
CHEMBL4202995 — Ki = 891.25 nM 6.05
CHEMBL4215197 — Ki = 891.25 nM 6.05
CHEMBL4217548 — Ki = 1243.0 nM 5.91
CHEMBL4217548 — Ki = 1230.27 nM 5.91
CHEMBL4211303 — Ki = 1412.54 nM 5.85
CHEMBL4211303 — Ki = 1407.0 nM 5.85
CHEMBL4203526 — Ki = 1436.0 nM 5.84
CHEMBL4203526 — Ki = 1445.44 nM 5.84
CHEMBL4202720 — pKi - — -
CHEMBL4202720 — Ki > 10000.0 nM -