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Assay Detail

CHEMBL3796374

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

Binding
Displacement of [125I]-Sar1,Ile8-angiotensin 2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting analysis
ChEMBL ↗
57
Total Activities
19
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

N-Phenyl indole derivatives as AT1 antagonists with anti-hypertension activities: Design, synthesis and biological evaluation.
Zhu W, Bao X, Ren H, Da Y, Wu D, Li F, Yan Y, Wang L, Chen Z.
Eur J Med Chem (2016) 115 : 161 -178
PubMed 27017546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.43 9.44
Ki 19 8.61 9.64
Activity 19 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3792453 — — 3 9.64
CHEMBL3794325 — — 3 9.17
CHEMBL3793734 — — 3 9.08
CHEMBL3793244 — — 3 8.94
CHEMBL3792439 — — 3 8.86
CHEMBL3793125 — — 3 8.79
CHEMBL3793558 — — 3 8.67
CHEMBL3792744 — — 3 8.63
CHEMBL3793122 — — 3 8.62
CHEMBL3794446 — — 3 8.59
CHEMBL1017 TELMISARTAN 4.0 3 8.56
CHEMBL3794276 — — 3 8.47
CHEMBL3793151 — — 3 8.39
CHEMBL3793287 — — 3 8.39
CHEMBL3794278 — — 3 8.33
CHEMBL3793939 — — 3 8.29
CHEMBL3793718 — — 3 8.15
CHEMBL3794502 — — 3 8.09
CHEMBL191 LOSARTAN 4.0 3 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3792453 — Ki = 0.23 nM 9.64
CHEMBL3792453 — IC50 = 0.36 nM 9.44
CHEMBL3794325 — Ki = 0.67 nM 9.17
CHEMBL3793734 — Ki = 0.84 nM 9.08
CHEMBL3794325 — IC50 = 0.92 nM 9.04
CHEMBL3793244 — Ki = 1.14 nM 8.94
CHEMBL3793734 — IC50 = 1.17 nM 8.93
CHEMBL3792439 — Ki = 1.39 nM 8.86
CHEMBL3793125 — Ki = 1.63 nM 8.79
CHEMBL3793244 — IC50 = 1.83 nM 8.74
CHEMBL3793558 — Ki = 2.12 nM 8.67
CHEMBL3792439 — IC50 = 2.23 nM 8.65
CHEMBL3792744 — Ki = 2.35 nM 8.63
CHEMBL3793122 — Ki = 2.37 nM 8.62
CHEMBL3794446 — Ki = 2.57 nM 8.59
CHEMBL3793125 — IC50 = 2.61 nM 8.58
CHEMBL1017 TELMISARTAN Ki = 2.75 nM 8.56
CHEMBL3793122 — IC50 = 3.27 nM 8.48
CHEMBL3793558 — IC50 = 3.39 nM 8.47
CHEMBL3794276 — Ki = 3.4 nM 8.47
CHEMBL3794446 — IC50 = 3.55 nM 8.45
CHEMBL3792744 — IC50 = 3.76 nM 8.43
CHEMBL1017 TELMISARTAN IC50 = 3.8 nM 8.42
CHEMBL3793287 — Ki = 4.06 nM 8.39
CHEMBL3793151 — Ki = 4.08 nM 8.39
CHEMBL3794278 — Ki = 4.66 nM 8.33
CHEMBL3794276 — IC50 = 4.7 nM 8.33
CHEMBL3793939 — Ki = 5.13 nM 8.29
CHEMBL3793287 — IC50 = 5.61 nM 8.25
CHEMBL3793151 — IC50 = 5.63 nM 8.25
CHEMBL3793718 — Ki = 7.06 nM 8.15
CHEMBL3794278 — IC50 = 7.46 nM 8.13
CHEMBL3794502 — Ki = 8.16 nM 8.09
CHEMBL3793939 — IC50 = 8.25 nM 8.08
CHEMBL3793718 — IC50 = 11.3 nM 7.95
CHEMBL191 LOSARTAN Ki = 13.06 nM 7.88
CHEMBL3794502 — IC50 = 13.06 nM 7.88
CHEMBL191 LOSARTAN IC50 = 20.09 nM 7.70
CHEMBL3792439 — Activity - — -
CHEMBL3794278 — Activity - — -
CHEMBL3793558 — Activity - — -
CHEMBL191 LOSARTAN Activity - — -
CHEMBL1017 TELMISARTAN Activity - — -
CHEMBL3794446 — Activity - — -
CHEMBL3794276 — Activity - — -
CHEMBL3793151 — Activity - — -
CHEMBL3793734 — Activity - — -
CHEMBL3793122 — Activity - — -
CHEMBL3793287 — Activity - — -
CHEMBL3794325 — Activity - — -