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Assay Detail

CHEMBL5340822

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Binding
Agonist activity at FXR-LBD (unknown origin) using fluorescein-coactivator peptide incubated for 3 hrs by TR-FRET assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bile acid receptor (CHEMBL2047) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Ren Q, Chen Y, Zhou Z, Cai Z, Jiao S, Huang W, Wang B, Chen S, Wang W, Cao Z, Yang Z, Deng L, Hu L, Zhang L, Li Z.
J Med Chem (2023) 66 : 6082 -6104
PubMed 37079895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.36 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318457 — — 1 7.19
CHEMBL5420029 — — 1 7.00
CHEMBL5419544 — — 1 6.91
CHEMBL5420532 — — 1 6.87
CHEMBL5396467 — — 1 6.84
CHEMBL5394417 — — 1 6.75
CHEMBL5437008 — — 1 6.68
CHEMBL5439401 — — 1 6.68
CHEMBL5401006 — — 1 6.64
CHEMBL5437656 — — 1 6.61
CHEMBL5419154 — — 1 6.58
CHEMBL5439051 — — 1 6.58
CHEMBL5418217 — — 1 6.57
CHEMBL5436041 — — 1 6.55
CHEMBL5435407 — — 1 6.52
CHEMBL5420842 — — 1 6.50
CHEMBL5432375 — — 1 6.42
CHEMBL5406213 — — 1 6.37
CHEMBL5429880 — — 1 6.33
CHEMBL5393982 — — 1 6.33
CHEMBL5417068 — — 1 6.30
CHEMBL5409694 — — 1 6.30
CHEMBL5407927 — — 1 6.21
CHEMBL5412521 — — 1 6.18
CHEMBL5413853 — — 1 6.14
CHEMBL5406838 — — 1 6.14
CHEMBL5411250 — — 1 6.11
CHEMBL5396259 — — 1 6.09
CHEMBL5394780 — — 1 6.08
CHEMBL5402010 — — 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318457 — EC50 = 65.0 nM 7.19
CHEMBL5420029 — EC50 = 100.0 nM 7.00
CHEMBL5419544 — EC50 = 122.0 nM 6.91
CHEMBL5420532 — EC50 = 135.0 nM 6.87
CHEMBL5396467 — EC50 = 143.0 nM 6.84
CHEMBL5394417 — EC50 = 180.0 nM 6.75
CHEMBL5437008 — EC50 = 209.0 nM 6.68
CHEMBL5439401 — EC50 = 209.0 nM 6.68
CHEMBL5401006 — EC50 = 231.0 nM 6.64
CHEMBL5437656 — EC50 = 244.0 nM 6.61
CHEMBL5439051 — EC50 = 261.0 nM 6.58
CHEMBL5419154 — EC50 = 260.0 nM 6.58
CHEMBL5418217 — EC50 = 270.0 nM 6.57
CHEMBL5436041 — EC50 = 283.0 nM 6.55
CHEMBL5435407 — EC50 = 302.0 nM 6.52
CHEMBL5420842 — EC50 = 320.0 nM 6.50
CHEMBL5432375 — EC50 = 381.0 nM 6.42
CHEMBL5406213 — EC50 = 423.0 nM 6.37
CHEMBL5429880 — EC50 = 468.0 nM 6.33
CHEMBL5393982 — EC50 = 465.0 nM 6.33
CHEMBL5409694 — EC50 = 506.0 nM 6.30
CHEMBL5417068 — EC50 = 503.0 nM 6.30
CHEMBL5407927 — EC50 = 624.0 nM 6.21
CHEMBL5412521 — EC50 = 656.0 nM 6.18
CHEMBL5413853 — EC50 = 718.0 nM 6.14
CHEMBL5406838 — EC50 = 721.0 nM 6.14
CHEMBL5411250 — EC50 = 781.0 nM 6.11
CHEMBL5396259 — EC50 = 811.0 nM 6.09
CHEMBL5394780 — EC50 = 830.0 nM 6.08
CHEMBL5402010 — EC50 = 854.0 nM 6.07
CHEMBL5408182 — EC50 = 916.0 nM 6.04
CHEMBL5422211 — EC50 = 926.0 nM 6.03
CHEMBL5422288 — EC50 = 1148.0 nM 5.94
CHEMBL5425382 — EC50 = 1286.0 nM 5.89
CHEMBL5440592 — EC50 = 1343.0 nM 5.87
CHEMBL5415126 — EC50 = 1423.0 nM 5.85
CHEMBL5408547 — EC50 = 1453.0 nM 5.84
CHEMBL5409448 — EC50 = 1574.0 nM 5.80
CHEMBL5416928 — EC50 > 10000.0 nM -
CHEMBL5408117 — EC50 > 10000.0 nM -
CHEMBL5420926 — EC50 > 10000.0 nM -
CHEMBL5405015 — EC50 > 10000.0 nM -
CHEMBL247920 — EC50 > 10000.0 nM -