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Assay Detail

CHEMBL809498

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

Binding
Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IM-9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL249) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
Hipskind PA, Howbert JJ, Bruns RF, Cho SS, Crowell TA, Foreman MM, Gehlert DR, Iyengar S, Johnson KW, Krushinski JH, Li DL, Lobb KL, Mason NR, Muehl BS, Nixon JA, Phebus LA, Regoli D, Simmons RM, Threlkeld PG, Waters DC, Gitter BD.
J Med Chem (1996) 39 : 736 -748
PubMed 8576917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 8.22 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42407 LANEPITANT 2.0 1 9.82
CHEMBL423623 — — 1 9.74
CHEMBL348976 — — 1 9.74
CHEMBL134500 — — 1 9.64
CHEMBL162337 — — 1 9.47
CHEMBL16192 CP-96345 — 1 9.46
CHEMBL352176 — — 1 9.10
CHEMBL350381 — — 1 9.09
CHEMBL351274 — — 1 9.07
CHEMBL353093 — — 1 9.01
CHEMBL554713 — — 1 8.96
CHEMBL165007 — — 1 8.93
CHEMBL350846 — — 1 8.89
CHEMBL350151 — — 1 8.81
CHEMBL165498 — — 1 8.72
CHEMBL350366 — — 1 8.70
CHEMBL163133 — — 1 8.66
CHEMBL164175 — — 1 8.60
CHEMBL106334 — — 1 8.56
CHEMBL350582 — — 1 8.55
CHEMBL165510 — — 1 8.52
CHEMBL163310 — — 1 8.52
CHEMBL351253 — — 1 8.51
CHEMBL162977 — — 1 8.49
CHEMBL165949 — — 1 8.49
CHEMBL166240 — — 1 8.40
CHEMBL166144 — — 1 8.35
CHEMBL423824 — — 1 8.34
CHEMBL423464 — — 1 8.28
CHEMBL165566 — — 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42407 LANEPITANT IC50 = 0.15 nM 9.82
CHEMBL423623 — IC50 = 0.18 nM 9.74
CHEMBL348976 — IC50 = 0.18 nM 9.74
CHEMBL134500 — IC50 = 0.23 nM 9.64
CHEMBL162337 — IC50 = 0.34 nM 9.47
CHEMBL16192 CP-96345 IC50 = 0.35 nM 9.46
CHEMBL352176 — IC50 = 0.8 nM 9.10
CHEMBL350381 — IC50 = 0.81 nM 9.09
CHEMBL351274 — IC50 = 0.85 nM 9.07
CHEMBL353093 — IC50 = 0.98 nM 9.01
CHEMBL554713 — IC50 = 1.1 nM 8.96
CHEMBL165007 — IC50 = 1.18 nM 8.93
CHEMBL350846 — IC50 = 1.28 nM 8.89
CHEMBL350151 — IC50 = 1.54 nM 8.81
CHEMBL165498 — IC50 = 1.9 nM 8.72
CHEMBL350366 — IC50 = 2.0 nM 8.70
CHEMBL163133 — IC50 = 2.2 nM 8.66
CHEMBL164175 — IC50 = 2.5 nM 8.60
CHEMBL106334 — IC50 = 2.73 nM 8.56
CHEMBL350582 — IC50 = 2.8 nM 8.55
CHEMBL165510 — IC50 = 3.0 nM 8.52
CHEMBL163310 — IC50 = 3.0 nM 8.52
CHEMBL351253 — IC50 = 3.1 nM 8.51
CHEMBL162977 — IC50 = 3.2 nM 8.49
CHEMBL165949 — IC50 = 3.2 nM 8.49
CHEMBL166240 — IC50 = 4.0 nM 8.40
CHEMBL166144 — IC50 = 4.5 nM 8.35
CHEMBL423824 — IC50 = 4.6 nM 8.34
CHEMBL423464 — IC50 = 5.3 nM 8.28
CHEMBL165566 — IC50 = 5.5 nM 8.26
CHEMBL166178 — IC50 = 7.2 nM 8.14
CHEMBL164563 — IC50 = 8.3 nM 8.08
CHEMBL353116 — IC50 = 9.2 nM 8.04
CHEMBL351940 — IC50 = 11.0 nM 7.96
CHEMBL162330 — IC50 = 21.9 nM 7.66
CHEMBL349273 — IC50 = 27.0 nM 7.57
CHEMBL423254 — IC50 = 27.4 nM 7.56
CHEMBL131171 — IC50 = 30.0 nM 7.52
CHEMBL165727 — IC50 = 31.0 nM 7.51
CHEMBL349882 — IC50 = 33.0 nM 7.48
CHEMBL162288 — IC50 = 51.0 nM 7.29
CHEMBL164912 — IC50 = 80.9 nM 7.09
CHEMBL433906 — IC50 = 85.0 nM 7.07
CHEMBL351922 — IC50 = 126.0 nM 6.90
CHEMBL163481 — IC50 = 149.0 nM 6.83
CHEMBL162636 — IC50 = 159.0 nM 6.80
CHEMBL165308 — IC50 = 338.0 nM 6.47
CHEMBL352102 — IC50 = 358.0 nM 6.45
CHEMBL351236 — IC50 = 420.0 nM 6.38
CHEMBL162332 — IC50 = 474.0 nM 6.32