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Assay Detail

CHEMBL4158376

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

Binding
Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assay
ChEMBL ↗
54
Total Activities
54
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

Endothelial PAS domain-containing protein 1 (CHEMBL1744522) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.
J Med Chem (2018) 61 : 9691 -9721
PubMed 30289716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.44 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161350 — — 1 8.00
CHEMBL4168513 — — 1 7.96
CHEMBL4173075 — — 1 7.92
CHEMBL4163990 — — 1 7.85
CHEMBL4176537 — — 1 7.80
CHEMBL4168978 — — 1 7.70
CHEMBL4161060 — — 1 7.70
CHEMBL4159016 — — 1 7.51
CHEMBL4168279 — — 1 7.50
CHEMBL4174407 — — 1 7.47
CHEMBL4169671 — — 1 7.39
CHEMBL4164468 — — 1 7.34
CHEMBL4167486 — — 1 7.31
CHEMBL4172344 — — 1 7.26
CHEMBL4167415 — — 1 7.22
CHEMBL4167439 — — 1 6.85
CHEMBL4162878 — — 1 6.85
CHEMBL4173593 — — 1 6.77
CHEMBL4164152 — — 1 6.75
CHEMBL4167600 — — 1 6.66
CHEMBL4172030 — — 1 6.55
CHEMBL4175480 — — 1 6.55
CHEMBL4170809 — — 1 6.46
CHEMBL4171869 — — 1 6.46
CHEMBL4164767 — — 1 6.34
CHEMBL2311933 — — 1 6.31
CHEMBL4169518 — — 1 6.16
CHEMBL4159573 — — 1 5.96
CHEMBL4160368 — — 1 5.92
CHEMBL4170828 — — 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161350 — IC50 = 10.0 nM 8.00
CHEMBL4168513 — IC50 = 11.0 nM 7.96
CHEMBL4173075 — IC50 = 12.0 nM 7.92
CHEMBL4163990 — IC50 = 14.0 nM 7.85
CHEMBL4176537 — IC50 = 16.0 nM 7.80
CHEMBL4168978 — IC50 = 20.0 nM 7.70
CHEMBL4161060 — IC50 = 20.0 nM 7.70
CHEMBL4159016 — IC50 = 31.0 nM 7.51
CHEMBL4168279 — IC50 = 32.0 nM 7.50
CHEMBL4174407 — IC50 = 34.0 nM 7.47
CHEMBL4169671 — IC50 = 41.0 nM 7.39
CHEMBL4164468 — IC50 = 46.0 nM 7.34
CHEMBL4167486 — IC50 = 49.0 nM 7.31
CHEMBL4172344 — IC50 = 55.0 nM 7.26
CHEMBL4167415 — IC50 = 60.0 nM 7.22
CHEMBL4167439 — IC50 = 140.0 nM 6.85
CHEMBL4162878 — IC50 = 140.0 nM 6.85
CHEMBL4173593 — IC50 = 170.0 nM 6.77
CHEMBL4164152 — IC50 = 180.0 nM 6.75
CHEMBL4167600 — IC50 = 220.0 nM 6.66
CHEMBL4172030 — IC50 = 280.0 nM 6.55
CHEMBL4175480 — IC50 = 280.0 nM 6.55
CHEMBL4170809 — IC50 = 350.0 nM 6.46
CHEMBL4171869 — IC50 = 350.0 nM 6.46
CHEMBL4164767 — IC50 = 460.0 nM 6.34
CHEMBL2311933 — IC50 = 490.0 nM 6.31
CHEMBL4169518 — IC50 = 700.0 nM 6.16
CHEMBL4159573 — IC50 = 1100.0 nM 5.96
CHEMBL4160368 — IC50 = 1200.0 nM 5.92
CHEMBL4170828 — IC50 = 1700.0 nM 5.77
CHEMBL4167896 — IC50 = 2400.0 nM 5.62
CHEMBL4160597 — IC50 = 3200.0 nM 5.50
CHEMBL4160172 — IC50 = 3600.0 nM 5.44
CHEMBL4175756 — IC50 = 4200.0 nM 5.38
CHEMBL4161430 — IC50 = 4200.0 nM 5.38
CHEMBL4172027 — IC50 = 4400.0 nM 5.36
CHEMBL4164839 — IC50 = 12700.0 nM 4.90
CHEMBL4177381 — IC50 = 18200.0 nM 4.74
CHEMBL4176171 — IC50 = 19600.0 nM 4.71
CHEMBL4170977 — IC50 = 22600.0 nM 4.65
CHEMBL4175477 — IC50 = 44400.0 nM 4.35
CHEMBL4163733 — IC50 = 52900.0 nM 4.28
CHEMBL4168682 — IC50 < 5.0 nM -
CHEMBL4159084 — IC50 > 100000.0 nM -
CHEMBL4162398 — IC50 < 5.0 nM -
CHEMBL4176457 — IC50 < 5.0 nM -
CHEMBL4165848 — IC50 < 5.0 nM -
CHEMBL4169277 — IC50 < 5.0 nM -
CHEMBL4172666 — IC50 < 5.0 nM -
CHEMBL4160209 — IC50 < 5.0 nM -