Ki Summary

Reaction Details

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Target

Diacylglycerol O-acyltransferase 1

Ligand

BDBM50003861

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1336096 (CHEMBL3240807)

IC50

15±n/a nM

Citation

Fox, BM; Sugimoto, K; Iio, K; Yoshida, A; Zhang, JK; Li, K; Hao, X; Labelle, M; Smith, ML; Rubenstein, SM; Ye, G; McMinn, D; Jackson, S; Choi, R; Shan, B; Ma, J; Miao, S; Matsui, T; Ogawa, N; Suzuki, M; Kobayashi, A; Ozeki, H; Okuma, C; Ishii, Y; Tomimoto, D; Furakawa, N; Tanaka, M; Matsushita, M; Takahashi, M; Inaba, T; Sagawa, S; Kayser, F Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents. J Med Chem57:3464-83 (2014) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Diacylglycerol O-acyltransferase 1

Name:

Diacylglycerol O-acyltransferase 1

Synonyms:

Type:

Protein

Mol. Mass.:

55297.82

Organism:

Homo sapiens (Human)

Description:

O75907

Residue:

488

Sequence:

MGDRGSSRRRRTGSRPSSHGGGGPAAAEEEVRDAAAGPDVGAAGDAPAPAPNKDGDAGVG
SGHWELRCHRLQDSLFSSDSGFSNYRGILNWCVVMLILSNARLFLENLIKYGILVDPIQV
VSLFLKDPYSWPAPCLVIAANVFAVAAFQVEKRLAVGALTEQAGLLLHVANLATILCFPA
AVVLLVESITPVGSLLALMAHTILFLKLFSYRDVNSWCRRARAKAASAGKKASSAAAPHT
VSYPDNLTYRDLYYFLFAPTLCYELNFPRSPRIRKRFLLRRILEMLFFTQLQVGLIQQWM
VPTIQNSMKPFKDMDYSRIIERLLKLAVPNHLIWLIFFYWLFHSCLNAVAELMQFGDREF
YRDWWNSESVTYFWQNWNIPVHKWCIRHFYKPMLRRGSSKWMARTGVFLASAFFHEYLVS
VPLRMFRLWAFTGMMAQIPLAWFVGRFFQGNYGNAAVWLSLIIGQPIAVLMYVHDYYVLN
YEAPAAEA

BDBM50003861

n/a

Name

BDBM50003861

Synonyms:

CHEMBL3235318

Type

Small organic molecule

Emp. Form.

C22H27N5O2

Mol. Mass.

393.4821

SMILES

CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(N)=O)CC1 |r,wU:19.21,wD:22.25,c:12,(42.45,-9.21,;40.91,-9.21,;41.68,-10.54,;39.58,-9.99,;38.25,-9.22,;36.91,-10,;35.58,-9.23,;35.58,-7.68,;36.91,-6.91,;36.9,-5.37,;38.24,-7.68,;39.57,-6.9,;40.91,-7.66,;42.24,-6.89,;43.57,-7.65,;44.9,-6.88,;44.89,-5.34,;43.54,-4.58,;42.22,-5.36,;46.22,-4.56,;46.19,-3.02,;47.53,-2.24,;48.87,-3,;50.2,-2.23,;51.54,-2.99,;51.55,-4.53,;52.87,-2.22,;48.87,-4.55,;47.55,-5.32,)|

Structure