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Assay Detail

CHEMBL4257110

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

Binding
Inhibition of human NHE3 expressed in OK cells assessed as reduction in Na+ dependent H+ antiport in presence of NHE1 inhibitor EIPA by BCECF-AM dye based fluorescence assay
169
Total Activities
169
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium/hydrogen exchanger 3 (CHEMBL3273)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nhe3-binding compounds and methods for inhibiting phosphate transport
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 169 7.56 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3942614 1 8.70
CHEMBL3987020 1 8.70
CHEMBL4283742 1 8.58
CHEMBL3950900 1 8.55
CHEMBL3954388 1 8.55
CHEMBL3937928 1 8.53
CHEMBL3921641 1 8.50
CHEMBL3972753 1 8.45
CHEMBL3968950 1 8.40
CHEMBL3956501 1 8.40
CHEMBL3967281 1 8.40
CHEMBL3923266 1 8.40
CHEMBL4279223 1 8.37
CHEMBL3976345 1 8.35
CHEMBL3979252 1 8.35
CHEMBL3906068 1 8.30
CHEMBL3304485 TENAPANOR 4.0 1 8.30
CHEMBL3891308 1 8.30
CHEMBL3911722 1 8.30
CHEMBL3909990 1 8.30
CHEMBL3903230 1 8.30
CHEMBL3972891 1 8.30
CHEMBL3965836 1 8.25
CHEMBL3949556 1 8.20
CHEMBL3946862 1 8.20
CHEMBL3913347 1 8.20
CHEMBL3954142 1 8.20
CHEMBL3908976 1 8.20
CHEMBL3908997 1 8.20
CHEMBL4280644 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3942614 IC50 = 1.995 nM 8.70
CHEMBL3987020 IC50 = 1.995 nM 8.70
CHEMBL4283742 IC50 = 2.63 nM 8.58
CHEMBL3950900 IC50 = 2.818 nM 8.55
CHEMBL3954388 IC50 = 2.818 nM 8.55
CHEMBL3937928 IC50 = 2.951 nM 8.53
CHEMBL3921641 IC50 = 3.162 nM 8.50
CHEMBL3972753 IC50 = 3.548 nM 8.45
CHEMBL3923266 IC50 = 3.981 nM 8.40
CHEMBL3968950 IC50 = 3.981 nM 8.40
CHEMBL3967281 IC50 = 3.981 nM 8.40
CHEMBL3956501 IC50 = 3.981 nM 8.40
CHEMBL4279223 IC50 = 4.266 nM 8.37
CHEMBL3976345 IC50 = 4.467 nM 8.35
CHEMBL3979252 IC50 = 4.467 nM 8.35
CHEMBL3304485 TENAPANOR IC50 = 5.012 nM 8.30
CHEMBL3906068 IC50 = 5.012 nM 8.30
CHEMBL3903230 IC50 = 5.012 nM 8.30
CHEMBL3909990 IC50 = 5.012 nM 8.30
CHEMBL3891308 IC50 = 5.012 nM 8.30
CHEMBL3911722 IC50 = 5.012 nM 8.30
CHEMBL3972891 IC50 = 5.012 nM 8.30
CHEMBL3965836 IC50 = 5.623 nM 8.25
CHEMBL3908997 IC50 = 6.31 nM 8.20
CHEMBL4280644 IC50 = 6.31 nM 8.20
CHEMBL3946862 IC50 = 6.31 nM 8.20
CHEMBL4289638 IC50 = 6.31 nM 8.20
CHEMBL3954142 IC50 = 6.31 nM 8.20
CHEMBL3949556 IC50 = 6.31 nM 8.20
CHEMBL3908976 IC50 = 6.31 nM 8.20
CHEMBL3913347 IC50 = 6.31 nM 8.20
CHEMBL4294068 IC50 = 7.413 nM 8.13
CHEMBL3911951 IC50 = 7.413 nM 8.13
CHEMBL4291672 IC50 = 7.943 nM 8.10
CHEMBL3972691 IC50 = 7.943 nM 8.10
CHEMBL3935315 IC50 = 7.943 nM 8.10
CHEMBL3951502 IC50 = 7.943 nM 8.10
CHEMBL3970997 IC50 = 7.943 nM 8.10
CHEMBL4284044 IC50 = 7.943 nM 8.10
CHEMBL3978115 IC50 = 7.943 nM 8.10
CHEMBL3985915 IC50 = 7.943 nM 8.10
CHEMBL3901000 IC50 = 10.0 nM 8.00
CHEMBL3897251 IC50 = 10.0 nM 8.00
CHEMBL3964147 IC50 = 10.0 nM 8.00
CHEMBL3930643 IC50 = 10.0 nM 8.00
CHEMBL3301627 TENAPANOR HYDROCHLORIDE IC50 = 10.0 nM 8.00
CHEMBL3908892 IC50 = 10.0 nM 8.00
CHEMBL3976660 IC50 = 10.0 nM 8.00
CHEMBL3941108 IC50 = 10.0 nM 8.00
CHEMBL3986598 IC50 = 11.75 nM 7.93