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Assay Detail

CHEMBL838642

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

Binding
Inhibitory constant for human cloned 5-HT4 receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.
Clark RD, Jahangir A, Alam M, Rocha C, Lin L, Bjorner B, Nguyen K, Grady C, Williams TJ, Stepan G, Tang HM, Ford AP.
Bioorg Med Chem Lett (2005) 15 : 1697 -1700
PubMed 15745824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 10.01 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180835 1 10.80
CHEMBL181202 1 10.60
CHEMBL361118 1 10.60
CHEMBL367354 1 10.50
CHEMBL182999 1 10.50
CHEMBL181126 1 10.50
CHEMBL180680 1 10.30
CHEMBL424790 1 10.30
CHEMBL180201 1 10.20
CHEMBL360449 1 10.10
CHEMBL360245 1 10.00
CHEMBL180830 1 10.00
CHEMBL178669 1 9.90
CHEMBL179833 1 9.90
CHEMBL178285 1 9.90
CHEMBL180697 1 9.80
CHEMBL181415 1 9.80
CHEMBL181928 1 9.70
CHEMBL180632 1 9.60
CHEMBL356359 PIBOSEROD 2.0 1 9.60
CHEMBL360531 1 9.60
CHEMBL179799 1 9.50
CHEMBL362582 1 9.40
CHEMBL182590 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180835 Ki = 0.01585 nM 10.80
CHEMBL181202 Ki = 0.02512 nM 10.60
CHEMBL361118 Ki = 0.02512 nM 10.60
CHEMBL367354 Ki = 0.03162 nM 10.50
CHEMBL182999 Ki = 0.03162 nM 10.50
CHEMBL181126 Ki = 0.03162 nM 10.50
CHEMBL180680 Ki = 0.05012 nM 10.30
CHEMBL424790 Ki = 0.05012 nM 10.30
CHEMBL180201 Ki = 0.0631 nM 10.20
CHEMBL360449 Ki = 0.07943 nM 10.10
CHEMBL360245 Ki = 0.1 nM 10.00
CHEMBL180830 Ki = 0.1 nM 10.00
CHEMBL178669 Ki = 0.1259 nM 9.90
CHEMBL179833 Ki = 0.1259 nM 9.90
CHEMBL178285 Ki = 0.1259 nM 9.90
CHEMBL180697 Ki = 0.1585 nM 9.80
CHEMBL181415 Ki = 0.1585 nM 9.80
CHEMBL181928 Ki = 0.1995 nM 9.70
CHEMBL180632 Ki = 0.2512 nM 9.60
CHEMBL356359 PIBOSEROD Ki = 0.2512 nM 9.60
CHEMBL360531 Ki = 0.2512 nM 9.60
CHEMBL179799 Ki = 0.3162 nM 9.50
CHEMBL362582 Ki = 0.3981 nM 9.40
CHEMBL182590 Ki = 0.7943 nM 9.10